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CTEP

Cat. No. M2542
CTEP  Structure
Synonym:

mGluR5 inhibitor

Size Price Availability Quantity
5mg USD 100  USD100 In stock
10mg USD 175  USD175 In stock
50mg USD 560  USD560 In stock
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Quality Control & Documentation
Biological Activity

CTEP (RO4956371) is a novel, long-acting, orally bioavailable allosteric antagonist of mGlu5 receptor with IC50 of 2.2 nM, shows >1000-fold selectivity over other mGlu receptors.

Chemical Information
Molecular Weight 391.77
Formula C19H13ClF3N3O
CAS Number 871362-31-1
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] David S Hong, et al. Larotrectinib in patients with TRK fusion-positive solid tumours: a pooled analysis of three phase 1/2 clinical trials

[2] Vivek Subbiah, et al. Advances in Targeting RET-Dependent Cancers

[3] Jared C Foster, et al. Single-Arm Phase II Trials of Combination Therapies: A Review of the CTEP Experience 2008-2017

[4] Haifeng Zhang, et al. CTEP Versus LESS Totally Extraperitoneal Hernioplasty

[5] Kieron Dunleavy, et al. Update on Burkitt Lymphoma

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  Catalog
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Keywords: CTEP , mGluR5 inhibitor supplier, GluR, inhibitors, activators


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