A GRP94 ligand
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GRP94 Inhibitor 1

Item No. 43140

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[(trans-4-hydroxycyclohexyl)amino]-4′-(1-methylethyl)-[1,1′-biphenyl]-3-carboxamide
CAS Number
2234897-35-7
Molecular Formula
C22H28N2O2
Formula Weight
352.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥ 10 mg/mlEthanol: Sparingly soluble: 1-10 mg/ml
SMILES
NC(C(C=C(C1=CC=C(C=C1)C(C)C)C=C2)=C2N[C@@H]3CC[C@H](CC3)O)=O
InChi Code
InChI=1S/C22H28N2O2/c1-14(2)15-3-5-16(6-4-15)17-7-12-21(20(13-17)22(23)26)24-18-8-10-19(25)11-9-18/h3-7,12-14,18-19,24-25H,8-11H2,1-2H3,(H2,23,26)/t18-,19-
InChi Key
JMGDXIHGWTVBMX-WGSAOQKQSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

Provide batch numbers separated by commas to download or request available product inserts, QC sheets, certificates of analysis, data packs, and GC-MS data.

    5 mg

    $54

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    10 mg

    $82

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    25 mg

    $190

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    50 mg

    $244

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    Product Description

    GRP94 inhibitor 1 is a ligand of glucose-regulated protein 94 (GRP94; IC50 = 2 nM in a fluorescence polarization assay).1 It decreases the levels of integrin α2 and integrin αL in PANC-1 cells when used at concentrations of 2.5 or 5 µM. GRP94 inhibitor 1 (10 or 30 mg/kg twice per day) increases body weight, decreases disease severity, and reduces serum and colon cell levels of TNF-α and IL-6 in a mouse model of ulcerative colitis induced by dextran sodium sulfate (DSS).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Jiang, F., Guo, A.-P., Xu, J.-C., et al. Discovery of a potent Grp94 selective inhibitor with anti-inflammatory efficacy in a mouse model of ulcerative colitis. J. Med. Chem. 61(21), 9513-9533 (2018).