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245728-44-3

245728-44-3 structure
245728-44-3 structure
  • Name: BTB09089
  • Chemical Name: GPR65 agonist
  • CAS Number: 245728-44-3
  • Molecular Formula: C14H12Cl2N4OS2
  • Molecular Weight: 387.307
  • Catalog: Research Areas Inflammation/Immunology
  • Create Date: 2021-12-20 18:28:26
  • Modify Date: 2024-01-02 07:10:49
  • 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].

Name GPR65 agonist
Synonyms 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
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
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.  

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