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抑制剂/激活剂

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凋亡与自噬

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G-1

G-1 是一个非甾体，高亲和力且有选择性的 GPR30 激动剂，其 Ki 值为 11 nM。

货号：
TK0619
规格：

1mg

5mg

10mg
价格：
￥0.00

产品参数

CAS No.	881639-98-1
生物活性	G-1 is a nonsteroidal, high-affinity and selective agonist of GPR30 with a Ki of 11 nM.
分子式	C21H18BrNO3
分子量	412.28
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	Powder -20°C 3 years
溶解性数据	DMSO : 50 mg/mL (121.28 mM; Need ultrasonic)
体内研究	The results at 14 days post-injury show that the Basso mouse scale (BMS) scores are significantly higher in the G-1 group compared with the other groups (P<0.05). The number of caspase-3-positive cells in the cross sections is counted, and G-1 group has fewer positive cells compare with the other groups (P<0.05), and there is no difference between the two groups (P>0.05). G-1 administration produces a statistically significant decrease in tumor volume from day 14 post treatment. Grafted tumors harvested after three-week treatment with G-1 show a significant decrease in tumor weight compare to vehicle treated animals.
体外研究	G-1 is a nonsteroidal, high-affinity and selective agonist of GPR30 with a Ki of 11 nM. Treatment with G-1 (10 μM and 100 μM) for 48 and 72 h significantly decreases cell proliferation (P<0.001). At 72 h, the IC50 value for G-1 is calculated to be 20 μM. Treatment of A549 cells with G-1 at a concentration of 20 μM reveals a significant increase in apoptosis, consistent with its antiproliferative effect (P<0.001). Cell cycle analysis of H295R cells after 24 h of G-1 treatment demonstrates a cell cycle arrest in the G2 phase. The presence of G-1 increases Bax expression while decreases Bcl-2.
文献	•J Cell Physiol. 2021 May;236(5):3780-3788. •Aging. 2020 Sep 13;12(17):17367-17379. •J Clin Endocrinol Metab. 2021 Feb 1;dgab020. •Phytomedicine. 2020 Mar;68:153146. •J Biochem Mol Toxicol. 2021 Feb;35(2):e22641. •Int J Endocrinol. 2021 Jun 18;2021:5575927. •J Histotechnol. 2021 Mar;44(1):27-36. •Research Square Preprint. 2021 Dec.
纯度及产品资料	98%

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