BTB09089

Names

[ Name ]:
BTB09089

[Synonym ]:
3-[(2,4-Dichlorobenzyl)sulfanyl]-1,6-dimethyl-1H-pyridazino[4,5-e][1,3,4]thiadiazin-5(6H)-one
1H-Pyridazino[4,5-e][1,3,4]thiadiazin-5(6H)-one, 3-[[(2,4-dichlorophenyl)methyl]thio]-1,6-dimethyl-
3-[(2,4-dichlorobenzyl)thio]-1,6-dimethyl-5,6-dihydro-1H-pyridazino[4,5-e][1,3,4]thiadiazin-5-one
MFCD00098495

Biological Activity

[Description]:

BTB09089 is a T cell death-associated gene 8 (TDAG8/GPR65) specific agonist. BTB09089 increases TDAG8 expression and regulates the cytokine production of T cells and macrophages[1].

[Related Catalog]:

Signaling Pathways >> Others >> Others

Research Areas >> Inflammation/Immunology

Research Areas >> Neurological Disease

[Target]

TDAG8/GPR65[1]

[In Vitro]

BTB09089 (0-18 μM; 30 min) 显著增加瞬时表达 hTDAG8 和 mTDAG8 的 HEK293 细胞中 cAMP 的积累，但在对照 HEK293 细胞中无明显增加。BTB09089 不增加表达 hGPR4 的 HEK293 细胞中 cAMP 的积累，也不增加表达 hOGR1 的 HEK293 细胞中肌醇磷酸盐的积累[1]。 BTB09089 (0-18 μM; 30 min) 在 pH 7.0-7.9 时显著地以剂量依赖的方式增强 cAMP 的积累，但在 pH 6.5 时则没有[1]。 BTB09089 (1-5 μM; 20 h) 以剂量依赖的方式抑制 WT 小鼠脾细胞中 IL-2 的产生，但不抑制 TDAG8 KO 小鼠 IL-2，且不影响细胞活力[1]。 BTB09089 (1-5 μM; 18 h) 抑制 LPS (HY-D1056) 刺激的 TNF-α 和 IL-6 的产生，并增强 LPS 刺激的硫酰乙酯诱导的腹膜渗出细胞 (TG-PEC) 中 IL-10 的产生[1]。

[In Vivo]

BTB09089 (5-20 μM, 8 μL; i.c.v.; 6 hours prior to MCAO) 减少大鼠脑缺血再灌注损伤[2]。 Animal Model: Adult male SD rats (270-280 g), middle cerebral artery occlusion (MCAO) model[2] Dosage: 5, 10 and 20 μM, 8 μL Administration: Intracerebroventricular injection, six hours prior to MCAO Result: Up-regulated TDAG8 and Bcl-2 expression and down-regulated cleaved caspase-3 expression, while the infarction volume was reduced, and neurological deficits were ameliorated 24 and 72 h after MCAO.

[References]

[1]. Onozawa Y, et al. Activation of T cell death-associated gene 8 regulates the cytokine production of T cells and macrophages in vitro. Eur J Pharmacol. 2012 May 15;683(1-3):325-31.

[2]. Ma XD, et al. TDAG8 activation attenuates cerebral ischaemia-reperfusion injury via Akt signalling in rats. Exp Neurol. 2017 Jul;293:115-123.

Chemical & Physical Properties

[ Density]:
1.6±0.1 g/cm3

[ Boiling Point ]:
500.6±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C₁₄H₁₂Cl₂N₄OS₂

[ Molecular Weight ]:
387.307

[ Flash Point ]:
256.6±32.9 °C

[ Exact Mass ]:
385.982971

[ LogP ]:
1.82

[ Vapour Pressure ]:
0.0±1.3 mmHg at 25°C

[ Index of Refraction ]:
1.733