CALP1 TFA

CALP1 TFA;

CALP1 TFA 是一种钙调蛋白 (CaM) 激动剂 (Kd 为 88 µM),与 CaM EF-hand/Ca2+ 结合位点结合。CALP1 TFA 通过抑制钙通道 (calcium channel) 的开放来阻止钙的流入和凋亡 (IC50 为 44.78 µM)。CALP1 TFA 阻止谷氨酸受体 ( glutamate receptor channels) 通道,并阻止存储操作的非选择性阳离子通道。CALP1 TFA 激活 CaM 依赖性磷酸二酯酶 (phosphodiesterase) 活性。

CALP1 TFAamp;;

CALP1 TFA Chemical Structure

规格 是否有货
100 mg ; 询价 ;
250 mg ; 询价 ;
500 mg ; 询价 ;

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生物活性

CALP1 TFA is a calmodulin (CaM) agonist (Kd of 88 µM) with binding to the CaM EF-hand/Ca2+-binding site. CALP1 TFA blocks calcium influx and apoptosis (IC50 of 44.78 µM) through inhibition of calcium channel opening. CALP1 TFA blocks glutamate receptor channels and blocks a store-operated nonselective cation channel. CALP1 TFA activates CaM-dependent phosphodiesterase activity[1][2][3][4].

IC50 Target

Kd: 88 µM (Calmodulin)[4]

分子量

956.10

Formula

C42H76F3N9O12

Sequence

Val-Ala-Ile-Thr-Val-Leu-Val-Lys

Sequence Shortening

VAITVLVK

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. R Houtman, et al. Attenuation of very late antigen-5-mediated adhesion of bone marrow-derived mast cells to fibronectin by peptides with inverted hydropathy to EF-hands. J Immunol. 2001 Jan 15;166(2):861-7.

    [2]. R Ten Broeke, et al. Calcium sensors as new therapeutic targets for airway hyperresponsiveness and asthma. FASEB J. 2001 Aug;15(10):1831-3.

    [3]. M K Manion, et al. A new type of Ca(2+) channel blocker that targets Ca(2+) sensors and prevents Ca(2+)-mediated apoptosis. FASEB J. 2000 Jul;14(10):1297-306.

    [4]. M Villain, et al. De novo design of peptides targeted to the EF hands of calmodulin. J Biol Chem. 2000 Jan 28;275(4):2676-85.

CALP1

CALP1;

CALP1 是一种钙调蛋白 (CaM) 激动剂 (Kd 为 88 µM),与 CaM EF-hand/Ca2+ 结合位点结合。CALP1 通过抑制钙通道 (calcium channel) 的开放来阻止钙的流入和凋亡 (IC50 为 44.78 µM)。CALP1 阻止谷氨酸受体 ( glutamate receptor channels) 通道,并阻止存储操作的非选择性阳离子通道。CALP1 激活 CaM 依赖性磷酸二酯酶 (phosphodiesterase) 活性。

CALP1amp;;

CALP1 Chemical Structure

CAS No. : 145224-99-3

规格 是否有货
100 mg ; 询价 ;
250 mg ; 询价 ;
500 mg ; 询价 ;

* Please select Quantity before adding items.

生物活性

CALP1 is a calmodulin (CaM) agonist (Kd of 88 µM) with binding to the CaM EF-hand/Ca2+-binding site. CALP1 blocks calcium influx and apoptosis (IC50 of 44.78 µM) through inhibition of calcium channel opening. CALP1 blocks glutamate receptor channels and blocks a store-operated nonselective cation channel. CALP1 activates CaM-dependent phosphodiesterase activity[1][2][3][4].

IC50 Target

Kd: 88 µM (Calmodulin)[4]

分子量

842.08

Formula

C40H75N9O10

CAS 号

145224-99-3

Sequence

Val-Ala-Ile-Thr-Val-Leu-Val-Lys

Sequence Shortening

VAITVLVK

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. R Houtman, et al. Attenuation of very late antigen-5-mediated adhesion of bone marrow-derived mast cells to fibronectin by peptides with inverted hydropathy to EF-hands. J Immunol. 2001 Jan 15;166(2):861-7.

    [2]. R Ten Broeke, et al. Calcium sensors as new therapeutic targets for airway hyperresponsiveness and asthma. FASEB J. 2001 Aug;15(10):1831-3.

    [3]. M K Manion, et al. A new type of Ca(2+) channel blocker that targets Ca(2+) sensors and prevents Ca(2+)-mediated apoptosis. FASEB J. 2000 Jul;14(10):1297-306.

    [4]. M Villain, et al. De novo design of peptides targeted to the EF hands of calmodulin. J Biol Chem. 2000 Jan 28;275(4):2676-85.

CALP2

CALP2;

CALP2 是一种钙调蛋白 (CaM) 拮抗剂 (Kd 为 7.9 µM),以亲和力结合 CaM EF-hand/Ca2+ 结合位点。CALP2 抑制 CaM 依赖性磷酸二酯酶 (phosphodiesterase) 活性并增加细胞内 Ca2+ 浓度。CALP2 有效抑制粘附和脱粒。CALP2 还是肺泡巨噬细胞的强激活剂。

CALP2amp;;

CALP2 Chemical Structure

CAS No. : 261969-04-4

规格 是否有货
100 mg ; 询价 ;
250 mg ; 询价 ;
500 mg ; 询价 ;

* Please select Quantity before adding items.

CALP2 的其他形式现货产品:

CALP2 TFA

生物活性

CALP2 is a calmodulin (CaM) antagonist ( (Kd of 7.9 µM)) with high affinity for binding to the CaM EF-hand/Ca2+-binding site. CALP2 inhibits CaM-dependent phosphodiesterase activity and increases intracellular Ca2+ concentrations. CALP2 potently inhibits of adhesion and degranulation. CALP2 is also a strong activator of alveolar macrophages[1][2][3][4].

分子量

1357.70

Formula

C68H104N14O13S

CAS 号

261969-04-4

Sequence

Val-Lys-Phe-Gly-Val-Gly-Phe-Lys-Val-Met-Val-Phe

Sequence Shortening

VKFGVGFKVMVF

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. R Houtman, et al. Attenuation of very late antigen-5-mediated adhesion of bone marrow-derived mast cells to fibronectin by peptides with inverted hydropathy to EF-hands. J Immunol. 2001 Jan 15;166(2):861-7.

    [2]. R Ten Broeke, et al. Calcium sensors as new therapeutic targets for airway hyperresponsiveness and asthma. FASEB J. 2001 Aug;15(10):1831-3.

    [3]. Robert Ten Broeke, et al. Specific modulation of calmodulin activity induces a dramatic production of superoxide by alveolar macrophages. Lab Invest. 2004 Jan;84(1):29-40.

    [4]. M Villain, et al. De novo design of peptides targeted to the EF hands of calmodulin. J Biol Chem. 2000 Jan 28;275(4):2676-85.

CALP2 TFA

CALP2 TFA; 纯度: 98.48%

CALP2 TFA 是一种钙调蛋白 (CaM) 拮抗剂 (Kd 为 7.9 µM),以亲和力结合 CaM EF-hand/Ca2+ 结合位点。CALP2 TFA 抑制 CaM 依赖性磷酸二酯酶 (phosphodiesterase) 活性并增加细胞内 Ca2+ 浓度。CALP2 TFA 有效抑制粘附和脱粒。CALP2 TFA 还是肺泡巨噬细胞的强激活剂。

CALP2 TFAamp;;

CALP2 TFA Chemical Structure

规格 价格 是否有货 数量
5 mg ¥2000 In-stock
10 mg ¥3400 In-stock
50 mg ; 询价 ;
100 mg ; 询价 ;

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CALP2 TFA 相关产品

bull;相关化合物库:

  • Bioactive Compound Library Plus
  • Immunology/Inflammation Compound Library
  • Membrane Transporter/Ion Channel Compound Library
  • Metabolism/Protease Compound Library
  • Neuronal Signaling Compound Library
  • Reprogramming Compound Library
  • Anti-Alzheimer’s Disease Compound Library
  • Neurodegenerative Disease-related Compound Library
  • Anti-Colorectal Cancer Compound Library
  • Peptide Library

生物活性

CALP2 TFA is a calmodulin (CaM) antagonist (Kd of 7.9 µM) with high affinity for binding to the CaM EF-hand/Ca2+-binding site. CALP2 TFA inhibits CaM-dependent phosphodiesterase activity and increases intracellular Ca2+ concentrations. CALP2 TFA potently inhibits of adhesion and degranulation. CALP2 TFA is also a strong activator of alveolar macrophages[1][2][3][4].

分子量

1471.72

Formula

C70H105F3N14O15S

Sequence

Val-Lys-Phe-Gly-Val-Gly-Phe-Lys-Val-Met-Val-Phe

Sequence Shortening

VKFGVGFKVMVF

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Sealed storage, away from moisture

Powder -80deg;C 2 years
-20deg;C 1 year

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

溶解性数据
In Vitro:;

DMSO : 50 mg/mL (33.97 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.6795 mL 3.3974 mL 6.7948 mL
5 mM 0.1359 mL 0.6795 mL 1.3590 mL
10 mM 0.0679 mL 0.3397 mL 0.6795 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;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。

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。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

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

    Solubility: ≥ 2.5 mg/mL (1.70 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (1.70 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂:;10% DMSO ;; 90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (1.70 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (1.70 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

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

    Solubility: ≥ 2.5 mg/mL (1.70 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (1.70 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 MCE 网站选购。
参考文献
  • [1]. R Houtman, et al. Attenuation of very late antigen-5-mediated adhesion of bone marrow-derived mast cells to fibronectin by peptides with inverted hydropathy to EF-hands. J Immunol. 2001 Jan 15;166(2):861-7.

    [2]. R Ten Broeke, et al. Calcium sensors as new therapeutic targets for airway hyperresponsiveness and asthma. FASEB J. 2001 Aug;15(10):1831-3.

    [3]. Robert Ten Broeke, et al. Specific modulation of calmodulin activity induces a dramatic production of superoxide by alveolar macrophages. Lab Invest. 2004 Jan;84(1):29-40.

    [4]. M Villain, et al. De novo design of peptides targeted to the EF hands of calmodulin. J Biol Chem. 2000 Jan 28;275(4):2676-85.