Cyclopenta[c]pyrrole-2(1H)-carboxamide, hexahydro-N-(3-methoxy-1,2,4-thiadiazol-5-yl)-5-(methyl-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-, (3aα,5α,6aα)-

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Cyclopenta[c]pyrrole-2(1H)-carboxamide, hexahydro-N-(3-methoxy-1,2,4-thiadiazol-5-yl)-5-(methyl-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-, (3aα,5α,6aα)- Suppliers list
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Products Intro: Product Name:SHR0302
CAS:1445987-21-2
Purity:98% Package:10MG;50MG;100MG,1G,5G,10G.100G
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Products Intro: Product Name:SHR0302；ARQ252
CAS:1445987-21-2
Package:1 mg；1 mL * 10mM (in DMSO)；10 mg；100 mg；200 mg；25 mg；5 mg；50 mg Remarks:REAGENT;FOR LABORATORY USE ONLY
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Products Intro: Product Name:(3aR,5s,6aS)-N-(3-methoxy-1,2,4-thiadiazol-5-yl)-5-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)hexahydrocyclopenta[c]pyrrole-2(1H)-carboxamide
CAS:1445987-21-2
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Products Intro: Product Name:SHR0302
CAS:1445987-21-2
Purity:0.98 Package:10G:100G
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Products Intro: Product Name:ARQ252
CAS:1445987-21-2
Purity:98% HPLC Package:5mg，10mg，50mg，100mg，1g，5g
Cyclopenta[c]pyrrole-2(1H)-carboxamide, hexahydro-N-(3-methoxy-1,2,4-thiadiazol-5-yl)-5-(methyl-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-, (3aα,5α,6aα)- Basic information
Product Name:Cyclopenta[c]pyrrole-2(1H)-carboxamide, hexahydro-N-(3-methoxy-1,2,4-thiadiazol-5-yl)-5-(methyl-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-, (3aα,5α,6aα)-
Synonyms:ARQ252;(3aR,5s,6aS)-N-(3-methoxy-1,2,4-thiadiazol-5-yl)-5-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)hexahydrocyclopenta[c]pyrrole-2(1H)-carboxamide;Th17,SHR-0302,B-cell,Inhibitor,inhibit,arthritis,collagen,migration,hepatic,SHR0302,JAK1,phosphorylation,anti-proliferation,Apoptosis,SHR 0302,JAK1-STAT3,fibrosis,JAK,anti-inflammatory,Janus kinase;Cyclopenta[c]pyrrole-2(1H)-carboxamide, hexahydro-N-(3-methoxy-1,2,4-thiadiazol-5-yl)-5-(methyl-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-, (3aα,5α,6aα)-;rel-(3aR,5s,6aS)-N-(3-Methoxy-1,2,4-thiadiazol-5-yl)-5-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)hexahydrocyclopenta[c]pyrrole-2(1H)-carboxamide;SHR0302, 10 mM in DMSO;Ivarmacitinib;SHR0302
CAS:1445987-21-2
MF:C18H22N8O2S
MW:414.49
EINECS:
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Mol File:1445987-21-2.mol
Cyclopenta[c]pyrrole-2(1H)-carboxamide, hexahydro-N-(3-methoxy-1,2,4-thiadiazol-5-yl)-5-(methyl-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-, (3aα,5α,6aα)- Structure
Cyclopenta[c]pyrrole-2(1H)-carboxamide, hexahydro-N-(3-methoxy-1,2,4-thiadiazol-5-yl)-5-(methyl-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-, (3aα,5α,6aα)- Chemical Properties
density 1.507±0.06 g/cm3(Predicted)
pka11.81±0.40(Predicted)
form Solid
color Off-white to light yellow
Safety Information
MSDS Information
Cyclopenta[c]pyrrole-2(1H)-carboxamide, hexahydro-N-(3-methoxy-1,2,4-thiadiazol-5-yl)-5-(methyl-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-, (3aα,5α,6aα)- Usage And Synthesis
UsesIvarmacitinib (SHR0302) is a potent and orally active all members of the JAK family inhibitor, particularly JAK1. The selectivity of Ivarmacitinib for JAK1 is >10-fold for JAK2, 77-fold for JAK3, 420-fold for Tyk2. Ivarmacitinib inhibits JAK1-STAT3 phosphorylation and induces the apoptosis of hepatic stellate cells. Ivarmacitinib has anti-proliferative and anti-inflammatory effects[1][2].
in vivo

Ivarmacitinib (SHR0302; 0.3-3.0 mg/kg; intragastric administration; twice a day; for 14 days; male Sprague-Dawley (SD) rats) treatment suppresses the severity of AA rats by attenuating the arthritis index, arthritis global assessment and paw swelling degree, and alleviated histopathology of spleen and joint of AA rats[1].
Ivarmacitinib can inhibit the proliferation of T, B and fibroblast-like synoviocytes (FLS), and down-regulates cytokines TNF-α, IL-1β, IL-17 and antibody IgG1, IgG2a levels, and suppresses the proportion of Th17 and total B, and inhibits JAK1-STAT3 phosphorylation[1].

Animal Model:Male Sprague-Dawley (SD) rats (150-180 g) injected with complete Freund’s adjuvant (CFA)[1]
Dosage:0.3 mg/kg,1.0 mg/kg, 3.0 mg/kg
Administration:Intragastric administration; twice a day; for 14 days
Result:Suppressed the severity of adjuvant-induced arthritis (AA) rats by attenuating the arthritis index, arthritis global assessment and paw swelling degree, and alleviated histopathology of spleen and joint of AA rats.
IC 50JAK1; JAK2; JAK3; Tyk2
References[1] Huaxun Wu, et al. JAK1-STAT3 Blockade by JAK Inhibitor SHR0302 Attenuates Inflammatory Responses of Adjuvant-Induced Arthritis Rats and Decreases Th17 and Total B Cells. Joint Bone Spine. 2016 Oct;83(5):525-32. DOI:10.1016/j.jbspin.2015.09.002
[2] Yuan-Jing Gu, et al. Targeted Blockade of JAK/STAT3 Signaling Inhibits Proliferation, Migration and Collagen Production as Well as Inducing the Apoptosis of Hepatic Stellate Cells. Int J Mol Med. 2016 Sep;38(3):903-11. DOI:10.3892/ijmm.2016.2692
Cyclopenta[c]pyrrole-2(1H)-carboxamide, hexahydro-N-(3-methoxy-1,2,4-thiadiazol-5-yl)-5-(methyl-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-, (3aα,5α,6aα)- Preparation Products And Raw materials
Tag:Cyclopenta[c]pyrrole-2(1H)-carboxamide, hexahydro-N-(3-methoxy-1,2,4-thiadiazol-5-yl)-5-(methyl-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-, (3aα,5α,6aα)-(1445987-21-2) Related Product Information
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