RAR-RXR-Agonists-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/RAR_RXR.html RAR/RXRRetinoic acid receptors; Retinoid X receptorsThe nuclear retinoic acid receptors (RARs) are transcriptional transregulators, which control the expression of specific gene subsetssubsequently to ligand binding and to strictly controlled phosp

2、horylation processes. RARs consist of three subtypes, (NR1B1), (NR1B2) and (NR1B3), encoded by separate genes. RARs function as ligand-dependent transcriptional regulators, heterodimerizedwith retinoid X receptors (RXRs), which also consist of three types, NR2B1, (NR2B2) and (NR2B3). RARs play criti

3、cal roles in avariety of biological processes, including development, reproduction, immunity, organogenesis and homeostasis, as assessed byvitamin A-deficiency (VAD), pharmacological and genetic studies conducted in the mouse.Retinoid X receptor (RXR) belongs to a family of ligand-activated transcri

4、ption factors that regulate many aspects of metazoan life.A class of nuclear receptors requires RXR as heterodimerization partner for their function.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/RAR/RXR.html RAR/RXR HYPERLINK https:/www.MedChemE/Targets/RAR/RXR.html HYPERLINK https:/www.MedCh

5、emE/Targets/RAR/RXR.html Inhibitors, HYPERLINK https:/www.MedChemE/Targets/RAR/RXR.html HYPERLINK https:/www.MedChemE/Targets/RAR/RXR.html Agonists, HYPERLINK https:/www.MedChemE/Targets/RAR/RXR.html HYPERLINK https:/www.MedChemE/Targets/RAR/RXR.html Antagonists, HYPERLINK https:/www.MedChemE/Target

6、s/RAR/RXR.html HYPERLINK https:/www.MedChemE/Targets/RAR/RXR.html Activators HYPERLINK https:/www.MedChemE/Targets/RAR/RXR.html HYPERLINK https:/www.MedChemE/Targets/RAR/RXR.html & HYPERLINK https:/www.MedChemE/Targets/RAR/RXR.html HYPERLINK https:/www.MedChemE/Targets/RAR/RXR.html Modulators HYPERL

7、INK https:/www.MedChemE/_addition_-Talarozole.html (+)-Talarozole HYPERLINK https:/www.MedChemE/_addition_-Talarozole.html HYPERLINK https:/www.MedChemE/_-_-Talarozole.html (-)-TalarozoleCat. No.: HY-14802C Cat. No.: HY-14802D(+)-Talarozole is a potent inhibitor of retinoicacid metabolism extracted

8、from patent WO 1997049704A1.(-)-Talarozole is a potent inhibitor of retinoicacid metabolism extracted from patent WO 1997049704A1.Purity: 99.28%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 1 mg, 5 mg, 10 mg, 25 mg, 50 mgPurity: 98.02%Clinical Data: No Development ReportedSize: 10 mM 1 mL,

9、 1 mg, 5 mg, 10 mg, 25 mg, 50 mg HYPERLINK https:/www.MedChemE/11-cis-retinoic-acid-d5.html 11-cis-Retinoic HYPERLINK https:/www.MedChemE/11-cis-retinoic-acid-d5.html HYPERLINK https:/www.MedChemE/11-cis-retinoic-acid-d5.html Acid-d5 HYPERLINK https:/www.MedChemE/11-cis-retinoic-acid-d5.html HYPERLI

10、NK https:/www.MedChemE/11-hydroxysugiol.html 11-HydroxysugiolCat. No.: HY-14649S2 Cat. No.: HY-10721811-cis-Retinoic Acid-d5 is the deuterium labeledRetinoic acid. Retinoic acid is a metabolite ofvitamin A that plays important roles in cellgrowth, differentiation, and organogenesis.11-Hydroxysugiol

11、regulates the SUMOylation ofintracellular receptors by modulating RAR andvitamin D3 receptor (VDR).Purity: 98%Clinical Data: No Development ReportedSize: 500 g, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/16-hydroxytrametenolic-acid.html 16-Hyd

12、roxytrametenolic HYPERLINK https:/www.MedChemE/16-hydroxytrametenolic-acid.html HYPERLINK https:/www.MedChemE/16-hydroxytrametenolic-acid.html acid HYPERLINK https:/www.MedChemE/16-hydroxytrametenolic-acid.html HYPERLINK https:/www.MedChemE/9-cis-13-cis-retinoic-acid-d5.html 9-cis,13-cis-Retinoic HY

13、PERLINK https:/www.MedChemE/9-cis-13-cis-retinoic-acid-d5.html HYPERLINK https:/www.MedChemE/9-cis-13-cis-retinoic-acid-d5.html acid-d5Cat. No.: HY-N2992 Cat. No.: HY-15127S216-Hydroxytrametenolic acid, a naturaltriterpene, is a potential retinoid X receptor(RXR) selective agonist.9-cis,13-cis-Retin

14、oic acid-d5 is the deuteriumlabeled Isotretinoin. Isotretinoin(13-cis-Retinoic acid) is a medication used forthe treatment of severe acne.Purity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.Me

15、dChemE/9-cis-retinoic-acid.html 9-cis-Retinoic HYPERLINK https:/www.MedChemE/9-cis-retinoic-acid.html HYPERLINK https:/www.MedChemE/9-cis-retinoic-acid.html acid HYPERLINK https:/www.MedChemE/9-cis-retinoic-acid.html HYPERLINK https:/www.MedChemE/9-cis-retinoic-acid-d5.html 9-cis-Retinoic HYPERLINK

16、https:/www.MedChemE/9-cis-retinoic-acid-d5.html HYPERLINK https:/www.MedChemE/9-cis-retinoic-acid-d5.html acid-d5(ALRT1057) Cat. No.: HY-15128Cat. No.: HY-132334S9-cis-Retinoic acid (ALRT1057), a vitamin Aderivative, is a potent RAR/RXR agonist.9-cis-Retinoic acid induces apoptosis, regulatescell cy

17、cle and has anticancer, anti-inflammatoryand neuroprotection activities.9-cis-Retinoic acid-d5 (ALRT1057-d5) is thedeuterium labeled 9-cis-Retinoic acid.9-cis-Retinoic acid (ALRT1057), a vitamin Aderivative, is a potent RAR/RXR agonist.Purity: 95.15%Clinical Data: LaunchedSize: 5 mgPurity: 98%Clinic

18、al Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg HYPERLINK https:/www.MedChemE/ac-261066.html AC-261066 HYPERLINK https:/www.MedChemE/ac-261066.html HYPERLINK https:/www.MedChemE/AC-55649.html AC-55649Cat. No.: HY-108532 Cat. No.: HY-108526AC-261066 is a potent, orally available andisoform-se

19、lective retinoic acid beta2 (RARbeta2)receptor agonist, with a pEC of 8.0.50AC-55649 is a potent, highly isoform-selectiveagonist of human RAR2 receptor, with a pECof 6.9.50Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.93%Clinical Data: No Development ReportedSize: 10 m

20、M 1 mL, 5 mg, 10 mg, 25 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/acitretin.html Acitretin(Ro 10-1670) Cat. No.: HY-B0107 HYPERLINK https:/www.MedChemE/Acitretin-sodium.html Acitretin HYPERLINK https:/www.MedChemE/Acitretin-sodium.html HYPERLINK https

21、:/www.MedChemE/Acitretin-sodium.html sodium(Ro 10-1670 sodium) Cat. No.: HY-B0107AAcitretin (Ro 10-1670) is a second-generation,systemic retinoid that has been used in thetreatment of psoriasis. Acitretin also can be usedfor the research of Alzheimers disease.Acitretin (Ro 10-1670) sodium is asecond

22、-generation, systemic retinoid that has beenused in the treatment of psoriasis. Acitretinsodium also can be used for the research ofAlzheimers disease.Purity: 99.79%Clinical Data: LaunchedSize: 10 mM 1 mL, 100 mg, 200 mg, 500 mgPurity: 98%Clinical Data: LaunchedSize: 1 mg, 5 mg HYPERLINK https:/www.

23、MedChemE/acitretin-d3.html Acitretin-d3(Ro 10-1670-d3) Cat. No.: HY-B0107S HYPERLINK https:/www.MedChemE/adapalene.html Adapalene(CD271) Cat. No.: HY-B0091Acitretin-d3 (Ro 10-1670-d3) is the deuteriumlabeled Acitretin. Acitretin (Ro 10-1670) is asecond-generation, systemic retinoid that has beenused

24、 in the treatment of psoriasis. Acitretin alsocan be used for the research of Alzheimersdisease.Adapalene (CD271), a third-generation syntheticretinoid, is widely used for the research of acne.Adapalene is a potent RAR agonist, with AC s50of 2.3 nM, 9.3 nM, and 22 nM for RAR, RAR,RAR, respectively.P

25、urity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.0%Clinical Data: LaunchedSize: 10 mM 1 mL, 50 mg, 100 mg, 500 mg HYPERLINK https:/www.MedChemE/adapalene-sodium-salt.html Adapalene HYPERLINK https:/www.MedChemE/adapalene-sodium-salt.html HYPERLINK https:/www.MedChemE/adapal

26、ene-sodium-salt.html sodium HYPERLINK https:/www.MedChemE/adapalene-sodium-salt.html HYPERLINK https:/www.MedChemE/adapalene-sodium-salt.html salt(CD 271 sodium salt) Cat. No.: HY-B0091A HYPERLINK https:/www.MedChemE/adapalene-d3.html Adapalene-d3Cat. No.: HY-B0091SAdapalene (CD271) sodium salt, a t

27、hird-generationsynthetic retinoid, is widely used for theresearch of acne. Adapalene sodium salt is apotent RAR agonist, with AC s of 2.3 nM, 9.350nM, and 22 nM for RAR, RAR, RAR,respectively.Adapalene-d3 is the deuterium labeled Adapalene.Adapalene (CD271), a third-generation syntheticretinoid, is

28、widely used for the research of acne.Adapalene is a potent RAR agonist, with AC s50of 2.3 nM, 9.3 nM, and 22 nM for RAR, RAR,RAR, respectively.Purity: 98%Clinical Data: LaunchedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 10 mg HYPERLINK https:/www.MedChemE/adapalene-

29、d6-methyl-ester.html Adapalene-d6 HYPERLINK https:/www.MedChemE/adapalene-d6-methyl-ester.html HYPERLINK https:/www.MedChemE/adapalene-d6-methyl-ester.html Methyl HYPERLINK https:/www.MedChemE/adapalene-d6-methyl-ester.html HYPERLINK https:/www.MedChemE/adapalene-d6-methyl-ester.html Ester HYPERLINK

30、 https:/www.MedChemE/adapalene-d6-methyl-ester.html HYPERLINK https:/www.MedChemE/agn-192870.html AGN HYPERLINK https:/www.MedChemE/agn-192870.html HYPERLINK https:/www.MedChemE/agn-192870.html 192870Cat. No.: HY-B0091S1 Cat. No.: HY-105689Adapalene-d6 Methyl Ester is the deuterium labeledAdapalene.

31、 Adapalene (CD271), a third-generationsynthetic retinoid, is widely used for theresearch of acne. Adapalene is a potent RARagonist, with AC s of 2.3 nM, 9.3 nM, and 22 nM50for RAR, RAR, RAR, respectively.AGN 192870 is a RAR neutral antagonist with K sdof 147, 33, and 42 nM for RAR, RAR, and RAR,resp

32、ectively. AGN 192870 shows IC s of 87 and 3250nM for RARand RAR, respectively. AGN 192870shows RAR partial agonism.Purity: 98%Clinical Data: No Development ReportedSize: 10 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/AGN_193109.html AGN H

33、YPERLINK https:/www.MedChemE/AGN_193109.html HYPERLINK https:/www.MedChemE/AGN_193109.html 193109 HYPERLINK https:/www.MedChemE/AGN_193109.html HYPERLINK https:/www.MedChemE/agn-193109-d7.html AGN HYPERLINK https:/www.MedChemE/agn-193109-d7.html HYPERLINK https:/www.MedChemE/agn-193109-d7.html 19310

34、9-d7Cat. No.: HY-U00449 Cat. No.: HY-U00449SAGN 193109 is a retinoid analog, and acts as aspecific and highly effective antagonist ofretinoic acid receptors (RARs), with K s of 2dnM, 2 nM, and 3 nM for RAR, RAR, and RAR,respectively.AGN 193109-d7 is the deuterium labeled AGN 193109.AGN 193109 is a r

35、etinoid analog, and acts as aspecific and highly effective antagonist ofretinoic acid receptors (RARs), with K s of 2dnM, 2 nM, and 3 nM for RAR, RAR, and RAR,respectively.Purity: 99.31%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mgPurity: 98%Clinical Data: No Development ReportedSiz

36、e: 1 mg, 10 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/AGN_194078.html AGN HYPERLINK https:/www.MedChemE/AGN_194078.html HYPERLINK https:/www.MedChemE/AGN_194078.html 194078Cat. No.: HY-100273 HYPERLINK https:/www.MedChemE/agn-194310.html AGN HYPERLINK https:/www.MedChemE/agn-194310.html HYPERLI

37、NK https:/www.MedChemE/agn-194310.html 194310(VTP-194310) Cat. No.: HY-16681AGN 194078 is a selective RAR agonist with aKd and EC50 of 3 and 112 nM, respectively.AGN 194310 (VTP-194310) is a high affinity, potentand selective retinioic acid receptors (RARs)pan-antagonist with K values of 3 nM, 2 nM,

38、 5 nMdfor RAR, RAR, RAR, respectively.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg, 25 mg, 50 mgPurity: 98.01%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg, 25 mg, 50 mg HYPERLINK https:/www.MedChemE/AGN-196996.html AGN HYPERLINK https:/www.MedChemE/AGN-19

39、6996.html HYPERLINK https:/www.MedChemE/AGN-196996.html 196996 HYPERLINK https:/www.MedChemE/AGN-196996.html HYPERLINK https:/www.MedChemE/agn-205327.html AGN HYPERLINK https:/www.MedChemE/agn-205327.html HYPERLINK https:/www.MedChemE/agn-205327.html 205327Cat. No.: HY-16682 Cat. No.: HY-16685AGN 19

40、6996 is a potent and selective RARantagonist with Ki value of 2 nM; little bindingaffinity for RAR(Ki=1087 nM) and RAR(Ki=8523nM).AGN 205327 is a potent synthetic RARs agonist withEC50 of 3766/734/32 nM for RAR/ respectively;no inhibition on RXR. IC50 value: 3766/734/32 nMfor RAR/ Target: RAR agonis

41、t.Purity: 99.37%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/AGN-205728.html AGN HYPERLINK https:/www.MedChemE/AGN-205728.html HYPERLINK https:/www.MedChemE/AGN-205728.html 205728Cat. No.: HY-166

42、83 HYPERLINK https:/www.MedChemE/AGN-195183.html AGN-195183(IRX-5183; VTP-195183; NRX-195183) Cat. No.: HY-16684AGN 205728 is a potent and selective RARantagonist with Ki/IC95 values of 3 nM/ 0.6 nM; noinhibiton on RAR and RAR. IC50 value: 3 nM/ 0.6nM(Ki/IC95) Target: RAR antagonist Moreinformation

43、can be found in the following patent,Compound 7a.AGN-195183 (IRX-5183) is a potent and selectiveagonist of RAR (K =3 nM) with improved bindingdselectivity relative to AGN 193836. AGN-195183 hasno activity on RAR/.Purity: 96.66%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.76%Clini

44、cal Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg HYPERLINK https:/www.MedChemE/agn194204.html AGN194204 HYPERLINK https:/www.MedChemE/agn194204.html HYPERLINK https:/www.MedChemE/AM580.html AM580(IRX4204; NRX194204; VTP 194204) Cat. No.: HY-13717 (CD336; NSC608001; Ro 40-

45、6055) Cat. No.: HY-10475AGN194204 (IRX4204) is an orally active andselective RXR agonist with K values 0.4 nM,d3.6 nM and 3.8 nM and EC s of 0.2 nM, 0.8 nM50and 0.08 nM for RXR, RXR and RXR,respectively. AGN194204 is inactive against RAR.AM580 is a selective RAR agonist with IC and50EC of 8 nM and 0

46、.36 nM, respectively.50Purity: 99.0%Clinical Data: Phase 2Size: 1 mg, 5 mgPurity: 99.61%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/amsilarotene.html Amsilarotene HYPERLINK https:/www.MedChemE/amsilarotene.html HYPERLINK https:/www

47、.MedChemE/AR7.html AR7(TAC-101; Am 555S) Cat. No.: HY-14653Cat. No.: HY-101106Amsilarotene (TAC-101; Am 555S), an orally activesynthetic retinoid, has selective affinity forretinoic acid receptor (RAR-) binding with Kiof 2.4, 400 nM for RAR- and RAR-.AR7 is an atypical RARA/RAR (retinoic acidrecepto

48、r, alpha) antagonist. AR7 specificallyactivates chaperone-mediated-autophagy (CMA)activity without affecting macroautophagy.Purity: 99.70%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98.85%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25

49、 mg, 50 mg, 100 mg4 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/atra-biotin.html ATRA-biotin(Biotin-ATRA-conjugate) Cat. No.: HY-141793 HYPERLINK https:/www.MedChemE/Bexarotene.html Bexarotene(LGD1069) Cat. No.: HY-14171ATRA-biotin (Biotin-ATRA-conjugate) i

50、s abiotin-conjugated ATRA. ATRA-biotin can be used totrack ATRA in cells or a given tissue.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgBexarotene (LGD1069) is a high-affinity andselective retinoid X receptors(RXR) agonist with EC s of 33, 24, 2550nM for RXR, RXR, and RXR, respec

51、tively.Bexarotene shows limited affinity for RARreceptors (EC 10000 nM).50Purity: 99.90%Clinical Data: LaunchedSize: 10 mM 1 mL, 50 mg, 100 mg, 500 mg HYPERLINK https:/www.MedChemE/bexarotene-d4.html Bexarotene HYPERLINK https:/www.MedChemE/bexarotene-d4.html HYPERLINK https:/www.MedChemE/bexarotene

52、-d4.html D4(LGD1069 D4) Cat. No.: HY-14171S HYPERLINK https:/www.MedChemE/bexarotene-d3.html Bexarotene-d3Cat. No.: HY-14171S1Bexarotene D4 is a deuterium labeled Bexarotene(LGD1069). Bexarotene (LGD1069) is a selectiveretinoid X receptors (RXR) agonist for thetreatment of cutaneous T-cell lymphoma.

53、Bexarotene-d3 (LGD1069-d3) is the deuteriumlabeled Bexarotene. Bexarotene (LGD1069) is ahigh-affinity and selective retinoid Xreceptors (RXR) agonist with EC s of5033, 24, 25 nM for RXR, RXR, and RXR,respectively.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Da

54、ta:Size: 2.5 mg, 1 mg, 5 mg, 10 mg HYPERLINK https:/www.MedChemE/bigelovin.html Bigelovin HYPERLINK https:/www.MedChemE/bigelovin.html HYPERLINK https:/www.MedChemE/bms-753.html BMS HYPERLINK https:/www.MedChemE/bms-753.html HYPERLINK https:/www.MedChemE/bms-753.html 753Cat. No.: HY-116506 Cat. No.:

55、 HY-107395Bigelovin, a sesquiterpene lactone isolated fromInula helianthus-aquatica, is a selective retinoidX receptor agonist. Bigelovin suppresses tumorgrowth through inducing apoptosis and autophagyvia the inhibition of mTOR pathway regulated byROS generation.BMS 753 is an isotype-selective retin

56、oic acidreceptor (RAR) agonist, with a K of 2 nM.iPurity: 99.81%Clinical Data: No Development ReportedSize: 5 mg, 10 mgPurity: 99.0%Clinical Data: No Development ReportedSize: 5 mg HYPERLINK https:/www.MedChemE/bms-195614.html BMS-195614 HYPERLINK https:/www.MedChemE/bms-195614.html HYPERLINK https:

57、/www.MedChemE/bms453.html BMS453(BMS 614) Cat. No.: HY-101259 (BMS-189453) Cat. No.: HY-100608BMS-195614 (BMS 614) is a neutral RAR-selectiveantagonist with a K of 2.5 nM.iBMS453 (BMS-189453), a synthetic retinoid, is aRAR agonist and a RAR/RAR antagonist. BMS453inhibits breast cell growth predomina

58、ntly throughthe induction of active TGF.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.89%Clinical Data: No Development ReportedSize: 5 mg HYPERLINK https:/www.MedChemE/bms493.html BMS493 HYPERLINK https:/www.MedChemE/bms493.html HYPERLINK https:/www.MedChemE/bms641.html

59、 BMS641Cat. No.: HY-108529(BMS-209641) Cat. No.: HY-119518BMS493 is an inverse pan-retinoic acid receptor(RAR) agonist. BMS493 increases nuclearcorepressor interaction with RARs. BMS493 alsocould prevent retinoic acid-induceddifferentiation.BMS641 (BMS-209641) is a selective RAR agonist.BMS641 has a

60、 higher affinity for RAR (K , 2.5dnM) that is 100 times higher than that for RAR(K , 225 nM) or RAR (K , 223 nM).d dPurity: 98.46%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgwww.MedChemE 5 HYPERLINK htt