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Ivarmacitinib
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Ivarmacitinib图片
CAS NO:1445987-21-2
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议

产品名称
SHR0302
产品介绍
Ivarmacitinib (SHR0302) 是一种有效的具有口服活性的JAK抑制剂,尤其是JAK1的抑制剂。Ivarmacitinib 对JAK1的选择性是JAK2的 10 倍以上,是JAK3的 77 倍,是Tyk2的 420 倍。Ivarmacitinib 抑制JAK1-STAT3磷酸化并诱导肝星状细胞凋亡 (apoptosis)。Ivarmacitinib 具有抗增殖和抗炎作用。
生物活性

Ivarmacitinib (SHR0302) is a potent and orally active all members of theJAKfamilyinhibitor, particularlyJAK1. The selectivity of Ivarmacitinib forJAK1is >10-fold forJAK2, 77-fold forJAK3, 420-fold forTyk2. Ivarmacitinib inhibitsJAK1-STAT3phosphorylation and induces theapoptosisof hepatic stellate cells. Ivarmacitinib has anti-proliferative and anti-inflammatory effects[1][2].

IC50& Target[1]

JAK1

 

JAK2

 

JAK3

 

Tyk2

 

体外研究
(In Vitro)

Ivarmacitinib (SHR0302; 1 nM-10 μM; 48 hours; HSCs) treatment displays an inhibitory effect on the proliferation of HSCs in a concentration-dependent manner[2].
Ivarmacitinib (1 nM-10 μM) exerts an inhibitory effect on the activation, proliferation and migration of HSCs[2].
Ivarmacitinib (1 nM-10 μM; 48 hours; HSCs) treatment induces the apoptosis of HSCs[2].
Ivarmacitinib (1 nM-10 μM; 48 hours; HSCs) treatment significantly increases the activation of caspase-3 and Bax in HSCs, and decreases the expression of Bcl-2. SHR0302 also inhibits the activation of Akt signaling pathway[2].

Cell Proliferation Assay[2]

Cell Line:Hepatic stellate cells (HSCs)
Concentration:1 nM, 10 nM, 100 nM, 1μM, 10 μM
Incubation Time:48 hours
Result:Displayed an inhibitory effect on the proliferation of HSCs, and that inhibition ocurred in a concentration-dependent manner.

Apoptosis Analysis[2]

Cell Line:Hepatic stellate cells (HSCs)
Concentration:1 nM, 10 nM, 100 nM, 1μM, 10 μM
Incubation Time:48 hours
Result:Induced the apoptosis of HSCs.

Western Blot Analysis[2]

Cell Line:Hepatic stellate cells (HSCs)
Concentration:1 nM, 10 nM, 100 nM, 1μM, 10 μM
Incubation Time:48 hours
Result:Significantly increased the activation of caspase-3 and Bax in HSCs, and decreased the expression of Bcl-2. Also inhibited the activation of Akt signaling pathway.
体内研究
(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.
Clinical Trial
分子量

414.48

性状

Solid

Formula

C18H22N8O2S

CAS 号

1445987-21-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 31.25 mg/mL(75.40 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.4127 mL12.0633 mL24.1266 mL
5 mM0.4825 mL2.4127 mL4.8253 mL
10 mM0.2413 mL1.2063 mL2.4127 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40%PEG300   5%Tween-80   45% saline

    Solubility: ≥ 2.08 mg/mL (5.02 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.02 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20%SBE-β-CDin saline)

    Solubility: ≥ 2.08 mg/mL (5.02 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.02 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90%corn oil

    Solubility: ≥ 2.08 mg/mL (5.02 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.02 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在本网站选购。