| Identification | Back Directory | [Name]
GRP94 | [CAS]
2234897-35-7 | [Synonyms]
GRP94
Grp94 Inhibitor-1
[1,1'-Biphenyl]-3-carboxamide, 4-[(trans-4-hydroxycyclohexyl)amino]-4'-(1-methylethyl)- | [Molecular Formula]
C22H28N2O2 | [MDL Number]
MFCD32067891 | [MOL File]
2234897-35-7.mol | [Molecular Weight]
352.47 |
| Chemical Properties | Back Directory | [Boiling point ]
532.5±50.0 °C(Predicted) | [density ]
1.165±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 250 mg/mL (709.28 mM; Need ultrasonic) | [form ]
Solid | [pka]
15.08±0.40(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
Grp94 Inhibitor-1 is a potent, selective Grp94 inhibitor with an IC50 value of 2 nM, and over 1000-fold selectivity to Grp94 against Hsp90α[1]. | [in vivo]
Grp94 Inhibitor-1 (intraperitoneal injection,qid.; coadminbistration 10 mg/kg or 30 mg/kg; 8 days) does not attenuate the colon shortening, but decreases disease activity index (DAI) scores. It also TNFα and IL-6 levels in the serum and colonic tissues and significantly reduces the p65 expression in colonic tissues, especially those in the 30 mg/kg dose group[1]. | Animal Model: | C57BL/6 mice (male, 20-22 g)[1] | | Dosage: | 10 mg/kg or 30 mg/kg | | Administration: | Intraperitoneal injection,qid.; coadminbistration 10 mg/kg or 30 mg/kg | | Result: | Decreased disease activity index (DAI) scores in UC mices. |
| [IC 50]
GRP94: 2 nM (IC50) | [storage]
Store at -20°C | [References]
[1] Jiang F, et al. Discovery of a Potent Grp94 Selective Inhibitor with Anti-Inflammatory Efficacy in a Mouse Model of Ulcerative Colitis. J Med Chem. 2018 Nov 8;61(21):9513-9533. DOI:10.1021/acs.jmedchem.8b00800 |
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| Company Name: |
cjbscvictory
|
| Tel: |
13348960310 |
| Website: |
https://www.weikeqi-biotech.com/ |
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