(S)-IBD3540 | GCPII inhibitor | Probechem Biochemicals

Chemical Structure : (S)-IBD3540

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(S)-IBD3540 ((S)-IBD 3540, IBD3540 S-form)

货号: PC-38667Not For Human Use, Lab Use Only.

(S)-IBD3540 is a potent, gut-restricted and orally active small molecule glutamate carboxypeptidase II (GCPII) inhibitor with IC50 of 4 nM, demonstrates anti-colitis activity in both acute and chronic mouse colitis models.

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100 mg		Get quote

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生物&药学活性

(S)-IBD3540 is a potent, selective, gut-restricted and orally active small molecule glutamate carboxypeptidase II (GCPII) inhibitor with IC50 of 4 nM (human GCPII).

(S)-IBD3540 does not have any concerning off-target activities using the industry standard Eurofins CEREP SafetyScreen44 panel at 10 uM.

(S)-IBD3540 dispalys 150-fold enhanced potency relative to (R)-IBD3540 (IC50=600 nM).

(S)-IBD3540 exhibits enantiospecific inhibition corresponding to the absolute configuration of l-glutamate in the binding pocket.

(S)-IBD3540 achieves high colon concentrations with low systemic exposure in both normal and colitic mice.

(S)-IBD3540 (10, or 100 mg/kg, once daily by oral gavage) displays dose-dependent activity in the DSS colitis mouse model and has superior activity to constituents 2-PMPA and DCA.

(S)-IBD3540 (100 mg/kg, once daily by oral gavage) attenuates monocytic inflammation in DSS colitis mouse models.

(S)-IBD3540 is efficacious in established spontaneous chronic colitis in IL-10 knockout mice.

物理化学性质&存储条件

分子量	630.71
分子式	C31H51O11P
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	10 mM in DMSO
Chemical Name/SMILES	(2S)-5-((((4R)-4-((3R,5R,9S,10S,12S,13R,14S)-3,12-dihydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)pentanoyl)oxy)methoxy)-5-oxo-2-(phosphonomethyl)pentanoic acid

参考文献

1. Manisha Pradhan, et al. FASEB J. 2022 May;36 Suppl 1.
2. Diane E Peters, et al. Sci Transl Med. 2023 Aug 9;15(708):eabn7491.

(S)-IBD3540 ((S)-IBD 3540, IBD3540 S-form)

生物&药学活性

物理化学性质&存储条件

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(S)-IBD3540 ((S)-IBD 3540, IBD3540 S-form)

生物&药学活性

物理化学性质&存储条件

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