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)-

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)-
CAS No.: 1445987-21-2
Chemical 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;SHR0302;Ivarmacitinib;SHR0302, 10 mM in DMSO;(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;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;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)-;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
CBNumber: CB58190607
Molecular Formula: C18H22N8O2S
Formula Weight: 414.48
MOL File: 1445987-21-2.mol

More

Less

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)- Property

Density: 1.507±0.06 g/cm3(Predicted)
pka: 11.81±0.40(Predicted)
form: Solid
color: Off-white to light yellow

More

Less

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

More

Less

N-Bromosuccinimide Price

ChemScene

Product number: CS-0062969
Product name: SHR0302
Purity: 99.58%
Packaging: 5mg
Price: $800
Updated: 2021/12/16

ChemScene

Product number: CS-0062969
Product name: SHR0302
Purity: 99.58%
Packaging: 10mg
Price: $1300
Updated: 2021/12/16

More

Less

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,Usage,Production

Uses

Ivarmacitinib (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 50

JAK1; 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

Raw materials

Preparation Products

More

Less

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

China 32 United States 1 Global 33

Shanghai Lollane Biological Technology Co.,Ltd.

Tel: 021-52996696，15000506266 15000506266
Fax: +86-21-52996696
Country: China
ProdList: 4601
Advantage: 55

Shanghai Beckham Medical Technology Co., Ltd

Tel: 021-13816613772 13816613772
Fax: QQ: 12922499
Email: huahero21@sina.com
Country: China
ProdList: 969
Advantage: 55

ShangHai Biochempartner Co.,Ltd

Tel: 17754423994 17754423994
Fax: QQ:2853530913
Email: 2853530910@QQ.com
Country: China
ProdList: 8011
Advantage: 62

Shanghai Rechem science Co., Ltd.

Tel: 21-31433387 15618786686
Fax: QQ:1369748377
Email: sales@rechemscience.com
Country: China
ProdList: 2981
Advantage: 58

Shanghai Chaolan Chemical Technology Center

Tel: 021-QQ：65489617 15618227136
Fax: 21-5161 9052
Email: Sales@ATKchemical.com
Country: China
ProdList: 9328
Advantage: 58

Shanghai SuperLan Chemcial Technique Centre

Tel: 021-2022843681 15618226720
Fax: +86-21-51601218
Email: lucy@atkchemical.com
Country: China
ProdList: 10499
Advantage: 58

SuZhou Medinoah Co.,LTD.

Tel: 0512-69561983 13914027025
Fax: 0512-69561982
Email: zhang_q@medinoah.com
Country: China
ProdList: 3655
Advantage: 58

Fujian boshi pharmaceutical technology co. LTD

Tel: 0595-22008920; 18120708884
Email: 393612455@qq.com
Country: China
ProdList: 255
Advantage: 58

Chengdu Feibo Pharm Technology Co., Ltd

Tel: +86 028-84641798 15982321820
Email: abby@arkpharm.com
Country: China
ProdList: 10922
Advantage: 58

ChemeGen(Shanghai) Biotechnology Co.,Ltd.

Tel: 18818260767
Fax: QQ 3610331285
Email: sales@chemegen.com
Country: China
ProdList: 11218
Advantage: 58

1445987-21-2, 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)-Related Search:

SHR0302

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

Ivarmacitinib

SHR0302, 10 mM in DMSO

1445987-21-2

C18H22N8O2S