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OD36
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。
OD36图片
CAS NO:1638644-62-8
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
50mg电议

产品介绍
OD36 是一种RIPK2抑制剂,IC50为 5.3 nM。OD36 是一种大环抑制剂,可与ALK2激酶 ATP 口袋有效结合。OD36 靶向作用于 ALK2,KD为 37 nM。
生物活性

OD36 is aRIPK2inhibitor with anIC50of 5.3 nM. OD36 is a macrocyclic inhibitor with potent binding to theALK2kinase ATP pocket. OD36 shows ALK2-directed activity withKDs of 37 nM[1][2].

IC50& Target[1][2]

RIPK2

5.3 nM (IC50)

ACVR1

37 nM (Kd)

ACVR1

47 nM (IC50)

ALK2 R206H

22 nM (IC50)

体外研究
(In Vitro)

OD36 also inhibits ALK2 and ALK2 R206H with IC50s of 47 and 22 nM, respevtively[1].
OD36 shows activity against ALK1 with a KDof 90 nM[2].
OD36 potently antagonize mutant ALK2 signaling and osteogenic differentiation[2].
OD36 (0.1-1 μM; 24 h) efficiently inhibits BMP-6 (50 ng/mL)-induced p-Smad1/5 in KS483 cells[2].
Preincubation of fibrodysplasia ossificans progressiva (FOP) endothelial colony-forming cells (ECFCs) with OD36 (0.5 μM) completely prevents the activation of Smad1/5 and gene targets ID-1 and ID-3 in response to activin A[2].

Western Blot Analysis[2]

Cell Line:KS483 cells
Concentration:0.1, 0.2, and 1 μM
Incubation Time:
Result:Inhibited BMP-6 induced p-Smad1/5.
体内研究
(In Vivo)

OD36 (6.25 mg/kg; i.p.; once) alleviates inflammation in an acute peritonitis mice model[3].

Animal Model:C57BL/6 mice, muramyl dipeptide (MDP)-induced model of peritonitis[3]
Dosage:6.25 mg/kg
Administration:Intraperitoneal injection, 30 min prior to MDP
Result:Inhibited the recruitment of inflammatory cells to the peritoneum, specifically that of neutrophils, and, to a lesser extent, lymphocytes. Decreased RIPK2-specific genes as well as inflammatory cytokine and chemokine gene expression.
分子量

330.77

性状

Solid

Formula

C16H15ClN4O2

CAS 号

1638644-62-8

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 : 33.33 mg/mL(100.76 mM;ultrasonic and warming and heat to 60℃)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM3.0232 mL15.1162 mL30.2325 mL
5 mM0.6046 mL3.0232 mL6.0465 mL
10 mM0.3023 mL1.5116 mL3.0232 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。