245728-44-3
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
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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 |
| 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 |