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CID-1067700 (ML282)

Cat. No. M10268
CID-1067700 (ML282) Structure
Synonym:

CID-1067700

Size Price Availability Quantity
5mg USD 100  USD100 In stock
10mg USD 140  USD140 In stock
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Quality Control & Documentation
Biological Activity

CID-1067700 (ML282) is a competitive inhibitors of nucleotide binding by Ras-related GTPases with a Ki of 13 nM for Rab7. CID-1067700 (ML282) preventing BODIPY-linked GTP and GDP binding with EC50 values of 11.2 and 21 nM, respectively. CID-1067700 (0-40 μM) inhibits Rab7 activity, NF-κB activation as well as AID induction in B cells.

In vivo, CID-1067700 (16 mg/kg; i.p.) prevents disease development in lupus-prone mice by Rab7 inhibition, and reduces IgG-IC deposition in MRL/Faslpr/lpr mice.

Chemical Information
Molecular Weight 390.48
Formula C18H18N2O4S2
CAS Number 314042-01-8
Solubility (25°C) DMSO ≥ 60 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Yuan Qin, et al. Acta Pharmacol Sin. CID1067700, a late endosome GTPase Rab7 receptor antagonist, attenuates brain atrophy, improves neurologic deficits and inhibits reactive astrogliosis in rat ischemic stroke

[2] Tonika Lam, et al. J Immunol. Small Molecule Inhibition of Rab7 Impairs B Cell Class Switching and Plasma Cell Survival To Dampen the Autoantibody Response in Murine Lupus

[3] Jacob O Agola, et al. ACS Chem Biol. A competitive nucleotide binding inhibitor: in vitro characterization of Rab7 GTPase inhibition

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Keywords: CID-1067700 (ML282), CID-1067700 supplier, Ras, inhibitors, activators


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