1. GPCR/G Protein
  2. Bombesin Receptor
  3. BIM-26226

BIM-26226 是一种选择性胃泌素释放肽 (GRP) (IC50 = 6 nM) 和蛙皮素 (BN 受体) 拮抗剂。BIM-26226 拮抗 BN 或 GRP 刺激的淀粉酶释放,其 IC50 值分别为 0.3 nM 和 0.2 nM。BIM-26226 对偏好 GRP 的 BN 受体亚型具有特异性,且对 GRP 受体系统无干扰。BIM-26226 可诱导生长抑素受体的合成,但对肿瘤的生长没有显著影响。

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Custom Peptide Synthesis

BIM-26226

BIM-26226 Chemical Structure

CAS No. : 136207-23-3

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规格 价格 是否有货 数量
1 mg ¥1100
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5 mg ¥2800
In-stock
10 mg ¥4500
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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

BIM-26226 is a selective gastrin-releasing peptide receptor (GRPR) (IC50 = 6 nM) and bombesin receptor (BN receptor) antagonist. BIM-26226 antagonizes BN- or GRP-stimulated amylase release with IC50 values of 0.3 nM and 0.2 nM, respectively. BIM-26226 is specific for the GRP-preferring BN receptor subtype with no interference with GRP receptor system. BIM-26226 can induce the synthesis of somatostatin receptor but has no significant effect on tumor growth[1][2][3][4].

IC50 & Target

bombesin receptor[1]

体外研究
(In Vitro)

BIM-26226 (0.1 nM-1 μM, 24 h) 显著降低了原代培养的胰腺肿瘤细胞中 [3H] 腺苷的掺入[1]
BIM-26226 对偏好 GRP 的 BN 受体亚型具有特异性,且不能抑制 AR4-2J 细胞中放射性标记的 CCK-33、胃泌素-17 或 VI P 的结合[2]
BIM-26226 (0.1 μM) 能够阻断蛙皮素诱导的 Ca2+ 升高,但不能阻断蛙皮素的生长刺激作用[3]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

BIM-26226 (30 和 100 μg/kg, s.c., 每日三次共 14 天) 仅对 GRP 刺激的大鼠胰腺肿瘤有明显抑制作用,但本身对肿瘤几乎无生长影响[1]
BIM-26226 (100 μg/kg, s.c., 每日一次共 6 周) 诱导生长抑素受体的合成,但对结肠癌大鼠模型中的肿瘤生长无影响[3]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Azaserine (HY-B0919)-induced pancreatic acinar carcinoma model established in Lewis rats[1]
Dosage: 30 and 100 μg/kg
Administration: Subcutaneous injection (s.c.), 3 times daily for 14 consecutive days
Result: Reduced the contents of protein, RNA, amylase and trypsin.
Did not significantly affect pancreatic growth parameters.
Animal Model: Colon cancer model induced by DHD/K12 tumor cell line established in male BDIX rats (12 weeks old) [3]
Dosage: 100 μg/kg
Administration: Subcutaneous injection (s.c.), once daily for 6 weeks
Result: Significantly decreased gastrinemia.
Had no effect on bombesin binding sites kDs and affinity site number Bmax.
分子量

1075.09

Formula

C49H63F5N12O10

CAS 号
性状

固体

颜色

White to off-white

Sequence

{D-F5 Phe}-Gln-Trp-{D-Ala}-Val-Ala-His-Leu-OMe

Sequence Shortening

{D-F5 Phe}-QW-{D-Ala}-VAHL-OMe

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Sealed storage, away from moisture

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
细胞实验: 

DMSO 中的溶解度 : 100 mg/mL (93.02 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.9302 mL 4.6508 mL 9.3015 mL
5 mM 0.1860 mL 0.9302 mL 1.8603 mL
查看完整储备液配制表

* 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;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

完整储备液配制表

* 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;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 0.9302 mL 4.6508 mL 9.3015 mL 23.2539 mL
5 mM 0.1860 mL 0.9302 mL 1.8603 mL 4.6508 mL
10 mM 0.0930 mL 0.4651 mL 0.9302 mL 2.3254 mL
15 mM 0.0620 mL 0.3101 mL 0.6201 mL 1.5503 mL
20 mM 0.0465 mL 0.2325 mL 0.4651 mL 1.1627 mL
25 mM 0.0372 mL 0.1860 mL 0.3721 mL 0.9302 mL
30 mM 0.0310 mL 0.1550 mL 0.3101 mL 0.7751 mL
40 mM 0.0233 mL 0.1163 mL 0.2325 mL 0.5813 mL
50 mM 0.0186 mL 0.0930 mL 0.1860 mL 0.4651 mL
60 mM 0.0155 mL 0.0775 mL 0.1550 mL 0.3876 mL
80 mM 0.0116 mL 0.0581 mL 0.1163 mL 0.2907 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Inquiry Information

产品名称:
BIM-26226
目录号:
HY-P0039
需求量: