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VU0424238

VU0424238

Item no.	CS-0009173-50mg
Manufacturer	ChemScene
Amount	50mg
Category	Reagents & Chemicals Molecules
Type	Molecules
Specific against	other
ECLASS 10.1	32169090
ECLASS 11.0	32169090
UNSPSC	12000000
Similar products	1396337-04-4
Available
CAS	1396337-04-4
Purity	>98%
Formula	C16H12FN5O2
MWt	325.30
Solubility	H2O : < 0.1 mg/mL (insoluble); DMSO : 22.73 mg/mL (69.87 mM; Need ultrasonic)
Clinical Information	No Development Reported
Pathway	GPCR/G Protein; Neuronal Signaling
Target	mGluR; mGluR
Biological Activity	VU0424238 is a novel and selective mGlu5 antagonist with an IC₅₀ value of 11 nM (rat) and an IC₅₀ value of 14 nM (human). VU0424238 has an acceptable CNS penetration^[1]. In Vitro: VU0424238 with an IC₅₀ value of 14 nM in HEK293A cells. It also binding a known allosteric site with K_i value of 4.4 nM in HEK293A cells. In Vivo: VU0424238 had a clearance of 19.3 mL/min/kg in rats and demonstrates 50% mGlu5 PET ligand occupancy at an oral dose of 0.8 mg/kg in rats. Plus, it also had a clearance of 15.5 mL/min/kg in cynomolgus monkeys and demonstrates 50% mGlu5 PET ligand occupancy at an oral dose of 0.06 mg/kg in baboons^[1].

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All products are intended for research use only (RUO). Not for human, veterinary or therapeutic use.

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