THIP

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

THIP 对 GABAA 受体的 δ 亚基有很强的亲和力。 THIP 是一种功能选择性 GABAAR 配体，可激动 α4β1δ、α4β3δ，并弱拮抗 αβγ 和 α4β2δ GABAAR。

THIP has a strong affinity for the δ subunit of GABAA receptors. THIP is a functionally selective GABAAR ligand, agonistic to α4β1δ, α4β3δ, and weakly antagonistic to αβγ and α4β2δ GABAARs.

THIP (1 μM; 5 s) induces a robust tonic GABAA-mediated current in layer 2/3 neurons.THIP (1 μM; 1 s) shows no affect miniature IPSCs in layer 2/3 neurons.Cell Viability Assay Cell Line:Layer 2/3 neurons (from male postnatal day 13-19 C57BL/6 mice)Concentration:1 μM Incubation Time:5 s Result:Induced a tonic current of 43.2 pA.Cell Viability Assay Cell Line:Layer 2/3 neurons (from male postnatal day 13-19 C57BL/6 mice)Concentration:1 μM Incubation Time:1 s Result:Resulted in only minor changes in the amplitude and frequency of mIPSCs.

THIP (Gaboxadol) (0.5, 5.0 mg/kg; p.o.; single) shws a good oral utilization, with Fa values of 110% and 83% for dosage of 0.5 and 5.0 mg/kg, respectively. Animal Model:Sprague-Dawley rats (255-276 g).Dosage:2.5 mg/kg (for i.v.); 0.5 and 5.0 mg/kg (for p.o.).

Gaboxadol | Gaboxadolum

Others

Other Targets

PPARγ

——

——

64603-91-4

140.142

C6H8N2O2

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (356.79 mM)

Oc1noc2CNCCc12

——

(-20℃)

With Ice Pack

≥ 2 years