(1R,2S)-VU0155041 - ≥98% , CAS No.1263273-14-8

CAS: 1263273-14-8 Cat. No.: V649977 Formule: C₁₄H₁₅Cl₂NO₃ Poids moléculaire: 316.18 Numéro CE: 119-554-0

GRADE & PURITY ≥98%

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

Vue d’ensemble

(1R,2S)-VU0155041, Cis regioisomer of VU0155041, is a partial mGluR4 agonist with an EC 50 of 2.35 μM.

In Vitro

At both human and rat receptors, the Cis regioisomer of VU0155041 is similar in potency (798±58 nM at human mGluR4 and 693±140 nM at rat mGluR4). Conversely, the concentration-response curve for the Trans regioisomer (VU0155040) does not plateau at the maximum concentration tested. Fold-shift experiments at 30 μM of VU0155041 also shows that the Cis regioisomer is more effective at this concentration on both human and rat mGluR4. VU0155041, induces concentration-dependent shifts in the baseline when examined in fold shift experiments using the thallium flux assay. VU0155041 induces a response that reaches approximately 45% of the maximal glutamate response. VU0155041is a partial agonist of mGluR4 that activates the receptor by interacting with a site that is distinct from the glutamate binding site. VU0155041 exhibitsselectivity for mGluR4 relative to 67 different targets and does not affect the function of striatal NMDA receptors. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

VU0155041 is soluble in an aqueous vehicle and intracerebroventricular administration of 31 to 316 nM of VU0155041 dose-dependently decreases haloperidol-induced catalepsy and reserpine-induced akinesia in rats. VU0155041, at doses of 31 and 92 nmol, is also able to significantly decrease the cataleptic effects of haloperidol, and the effects of the compound are still present 30 min after infusion. Icv infusion of a 316 nmol dose of VU0155041 also results in a significant reversal of akinesia . MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Form:Solid

IC50& Target:mGluR4

Specifications

Spécifications et pureté

≥98%

Mécanismes biochimiques et physiologiques

(1R,2S)-VU0155041, Cis regioisomer of VU0155041, is a partial mGluR4 agonist with an EC 50 of 2.35 μM.

Conditions de stockage de stockage

Store at -20°C

Expédié en

Ice chest + Ice pads

Ce produit nécessite l'expédition en chaîne froide. Les services terrestres et autres services économiques ne sont pas disponibles.

Type d'action

AGONIST

Pureté

≥98%

Noms et identifiants

Poids moléculaire

316.18

Propriétés chimiques et physiques

• Solubilité: DMSO : 50 mg/mL (158.14 mM; Need ultrasonic)