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  3. G15

G15 

目录号: HY-103449 纯度: >99.0%
产品使用指南

G15 是一种高亲和力和选择性 G 蛋白偶联雌激素受体 (GPER/GPR30) 拮抗剂,Ki 值为 20 nM。

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G15 Chemical Structure

G15 Chemical Structure

CAS No. : 1161002-05-6

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Size Price Stock Quantity
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ¥935 In-stock
5 mg ¥850 In-stock
10 mg ¥1400 In-stock
50 mg ¥4300 In-stock
100 mg ¥7400 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Description

G15 is a high affinity and selective G-protein-coupled estrogen receptor (GPER/GPR30) antagonist with a Ki of 20 nM[1][2].

IC50 & Target

Ki: 20 nM (GPER/GPR30)[2]

In Vitro

G15 (0.1-10 μM; 2 days) inhibits GPER-mediated proliferation stimulated by 17β-estradiol (E2) in A549 and H1793 cell lines[1].
G15 (1 μM; 48 hours) inhibits the response of GPER stimulated by E2 and G1 in A549 and H1793 cell lines[1].

Cell Proliferation Assay[1]

Cell Line: A549, H1793 cell lines
Concentration: 0.1, 1, 10 μM (combination with 10 nM E2)
Incubation Time: 2 days
Result: Inhibited GPER-mediated proliferation stimulated by E2.

Western Blot Analysis[1]

Cell Line: A549, H1793 cell lines
Concentration: 1 μM (combination with 10 nM E2 and 10 nM G1)
Incubation Time: 48 hours
Result: Inhibited the response of GPER stimulated by E2 and G1.
In Vivo

G15 (1.46 mg/kg; i.h.; twice a week for 14 weeks) decreases the number of tumor nodules and tumor index increased by the E2 or G1 group in urethane-induced adenocarcinoma mice[1].

Animal Model: Four-week-old female Kunming mice (Urethane-induced adenocarcinoma)[1]
Dosage: 1.46 mg/kg (combination with E2, 0.09 mg/kg and fulvestrant (Ful), 2.4 mg/kg)
Administration: Subcutaneous injection; twice a week for 14 weeks
Result: The number of tumor nodules decreased in the E2+Ful+G15 group.
Clinical Trial
Molecular Weight

370.24

Formula

C₁₉H₁₆BrNO₂

CAS No.

1161002-05-6

SMILES

BrC1=C([C@@H]2NC3=C(C=CC=C3)[C@@]4([H])[C@]2([H])CC=C4)C=C5OCOC5=C1

Shipping

Room temperature in continental US; may vary elsewhere

Storage

-20°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 41.67 mg/mL (112.55 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7010 mL 13.5048 mL 27.0095 mL
5 mM 0.5402 mL 2.7010 mL 5.4019 mL
10 mM 0.2701 mL 1.3505 mL 2.7010 mL
* 请根据产品在不同溶剂中的溶解度,选择合适的溶剂配制储备液,并请注意储备液的保存方式和期限。
In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案,配制前请先配制澄清的储备液,再依次添加助溶剂 (为保证实验结果的可靠性,体内实验的工作
液,建议您现用现配,当天使用;澄清的储备液可以根据储存条件,适当保存;以下溶剂前的百分比是指该溶剂在您配制终溶液中的体积占比):

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (5.62 mM); Clear solution

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (5.62 mM); Clear solution

*以上所有助溶剂都可在 MCE 网站选购。
References

Purity: >99.0%

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

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产品名称:
G15
目录号:
HY-103449
需求量:

G15

Cat. No.: HY-103449