TASP0433864

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MedKoo CAT#: 530534

CAS#: 1431980-60-7

Description: TASP0433864 is a novel positive allosteric modulator of metabotropic glutamate 2 receptor. TASP0433864 exhibited PAM activity at human and rat mGlu2 receptors with EC50 values of 199 and 206 nM, respectively, without exerting agonist activity at rat mGlu2 receptor. TASP0433864 produced a leftward and upward shift in the concentration-response curve of glutamate-increased guanosine 5'-O-(3-[(35)S]thio)triphosphate binding to mGlu2 receptor. The inhibitory effect of TASP0433864 on cortical activation was also observed in the mouse 2-deoxy-glucose uptake study. TASP0433864 is a selective mGlu2 receptor PAM with antipsychotic activity, and the attenuation of excess glutamatergic neurotransmission may be involved in the action of TASP0433864.

Chemical Structure

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TASP0433864
CAS# 1431980-60-7
Instruction

Theoretical Analysis

MedKoo Cat#: 530534
Name: TASP0433864
CAS#: 1431980-60-7
Chemical Formula: C18H23N3O3
Exact Mass: 329.17
Molecular Weight: 329.400
Elemental Analysis: C, 65.63; H, 7.04; N, 12.76; O, 14.57

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

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Synonym: TASP0433864, TASP0433864, TASP0433864

IUPAC/Chemical Name: (2S)-2-[[4-(1,1-Dimethylethyl)phenoxy]methyl]-2,3-dihydro-5-methylimidazo[2,1-b]oxazole-6-carboxamide

InChi Key: IZYYTLCSQBACIP-AWEZNQCLSA-N

InChi Code: InChI=1S/C18H23N3O3/c1-11-15(16(19)22)20-17-21(11)9-14(24-17)10-23-13-7-5-12(6-8-13)18(2,3)4/h5-8,14H,9-10H2,1-4H3,(H2,19,22)/t14-/m0/s1

SMILES Code: O=C(C1=C(C)N2C(O[C@H](COC3=CC=C(C(C)(C)C)C=C3)C2)=N1)N

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 329.40 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Hiyoshi T, Marumo T, Hikichi H, Tomishima Y, Urabe H, Tamita T, Iida I, Yasuhara A, Karasawa J, Chaki S. Neurophysiologic and antipsychotic profiles of TASP0433864, a novel positive allosteric modulator of metabotropic glutamate 2 receptor. J Pharmacol Exp Ther. 2014 Dec;351(3):642-53. doi: 10.1124/jpet.114.218651. PubMed PMID: 25277141.