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CID-1067700 (ML282)

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

CID-1067700

Size Price Availability Quantity
5mg USD 90  USD100 In stock
10mg USD 126  USD140 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 390.48
Formula C18H18N2O4S2
CAS Number 314042-01-8
Purity >99%
Solubility DMSO ≥ 60 mg/mL
Storage at -20°C
References

CID1067700, a late endosome GTPase Rab7 receptor antagonist, attenuates brain atrophy, improves neurologic deficits and inhibits reactive astrogliosis in rat ischemic stroke
Yuan Qin, et al. Acta Pharmacol Sin. 2019 Jun;40(6):724-736. PMID: 30315251.

Small Molecule Inhibition of Rab7 Impairs B Cell Class Switching and Plasma Cell Survival To Dampen the Autoantibody Response in Murine Lupus
Tonika Lam, et al. J Immunol. 2016 Nov 15;197(10):3792-3805. PMID: 27742832.

A competitive nucleotide binding inhibitor: in vitro characterization of Rab7 GTPase inhibition
Jacob O Agola, et al. ACS Chem Biol. 2012 Jun 15;7(6):1095-108. PMID: 22486388.

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  Catalog
Abmole Inhibitor Catalog 2017




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

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