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首页-小分子抑制剂&激动剂-GPCR-Lysophospholipid Receptor-Icanbelimod
Icanbelimod

Chemical Structure : Icanbelimod

CAS No.: 1514888-56-2

Icanbelimod (CBP-307, CBP307)

货号: PC-42341Not For Human Use, Lab Use Only.

Icanbelimod (CBP-307) is a highly potent, next-generation highly potent sphingosine-1-phosphate receptor (S1PR) agonist with EC50 of 3.55 nM (S1PR1), specifically targets S1PR1/4/5.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Icanbelimod (CBP-307) is a highly potent, next-generation highly potent sphingosine-1-phosphate receptor (S1PR) agonist with EC50 of 3.55 nM (S1PR1), specifically targets S1PR1/4/5.
Icanbelimod (CBP-307) has significantly higher potency for S1PR1 than for S1PR4 and S1PR5, and no activity against S1PR2 and S1PR23.
Icanbelimod (CBP-307) has no notable activity for S1PR3 in Chinese hamster ovary cells expressing human S1PRs.
Icanbelimod (CBP-307) demonstrated large (>50%) reductions in lymphocyte counts and, notably, a short elimination half-life (5.3 hours in rats) when indirectly compared with fingolimod (23.4 hours) in vivo.
Icanbelimod (CBP-307) is currently being evaluated in a global phase 2 clinical study in moderate to severe ulcerative colitis and Crohn's disease.

物理化学性质&存储条件

分子量 409.4533632
分子式 C23H24FN3O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

DMSO: 6.8 mg/mL (Need ultrasonic and warming)

Chemical Name/SMILES

3-Azetidinecarboxylic acid, 1-[[2-fluoro-4-[5-[4-(2-methylpropyl)phenyl]-1,2,4-oxadiazol-3-yl]phenyl]methyl]-

参考文献

1. Patent WO 2015039587 A1.
2. Leiye Yu, et al. Proc Natl Acad Sci U S A. 2022 Apr 19;119(16):e2117716119.
3. Lickliter J, et al. Front Immunol. 2024 Jun 17;15:1380975.

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