Mastoparan (trifluoroacetate salt)
目录号 : GC47601
A neuropeptide with diverse biological activities
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Mastoparan is a mast cell degranulating peptide originally isolated from Vespid wasp venom.1 It promotes degranulation by increasing GTPase activity for Gi and Go signaling independent of G protein-coupled receptor binding.2,3 Mastoparan also binds calmodulin (Kd = 0.3 nM) and inhibits the calmodulin-induced activation of phosphodiesterase (IC50 = 0.02 µM).4,5 In vitro, mastoparan was effective in killing leukemia, myeloma, and breast cancer cells (IC50s = 8-9.2, 11, and 20-24 µM, respectively).6 It worked synergistically with gemcitabine in a mouse model of mammary carcinoma.6
1.Hirai, Y., Yashuhara, T., Yoshida, H., et al.A new mast cell degranulating peptide "mastoparan" in the venom of Vespula lewisiiChem. Pharm. Bull. (Tokyo)27(8)1942-1944(1979) 2.Higashijima, T., Uzu, S., Nakajima, T., et al.Mastoparan, a peptide toxin from wasp venom, mimics receptors by activating GTP-binding regulatory proteins (G proteins)J. Biol. Chem.263(14)6491-6494(1988) 3.Higashijima, T., Burnier, J., and Ross, E.M.Regulation of Gi and Go by mastoparan, related amphiphilic peptides, and hydrophobic amines. Mechanism and structural determinants of activityJ. Biol. Chem.265(24)14176-14186(1990) 4.Malencik, D.A., and Anderson, S.R.High affinity binding of the mastoparans by calmodulinBiochem. Biophys. Res. Commun.114(1)50-56(1983) 5.Barnette, M.S., Daly, R., and Weiss, B.Inhibition of calmodulin activity by insect venom peptidesBiochem. Pharmacol.32(19)2929-2933(1983) 6.Hilchie, A.L., Sharon, A.J., Haney, E.F., et al.Mastoparan is a membranolytic anti-cancer peptide that works synergistically with gemcitabine in a mouse model of mammary carcinomaBiochim Biophys. Acta.1858(12)3195-3204(2016)
| Cas No. | N/A | SDF | |
| Canonical SMILES | O=C(N[C@@H]([C@@H](C)CC)C(N[C@H](C(N)=O)CC(C)C)=O)[C@H](CCCCN)NC([C@H](CCCCN)NC([C@H](C)NC([C@H](CC(C)C)NC([C@H](C)NC([C@H](C)NC([C@H](CC(C)C)NC([C@H](C)NC([C@H](CCCCN)NC([C@H](CC(C)C)NC([C@H](CC(N)=O)NC([C@@H](N)[C@@H](C)CC)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O.FC(F)(C(O)=O)F | ||
| 分子式 | C70H131N19O15.XCF3COOH | 分子量 | 1478.9 |
| 溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 30 mg/ml,Ethanol:PBS (pH 7.2) (1:3): 0.25 mg/ml | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 0.6762 mL | 3.3809 mL | 6.7618 mL |
| 5 mM | 0.1352 mL | 0.6762 mL | 1.3524 mL |
| 10 mM | 0.0676 mL | 0.3381 mL | 0.6762 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Perchlorate-induced formation of the alpha-helical structure of Mastoparan
J Biochem 1994 Oct;116(4):910-5.PMID:7883768DOI:10.1093/oxfordjournals.jbchem.a124615
Mastoparan, a basic tetradecapeptide from wasp venom, has been considered to be unfolded under aqueous conditions. On the basis of the far-UV circular dichroism spectrum, we found that sodium perchlorate at molar concentrations stabilizes an alpha-helical structure of Mastoparan. To understand the mechanism of the perchlorate-induced stabilization of the alpha-helical structure, we synthesized a dimeric form of Mastoparan derivative, which was linked at the C terminal by a disulfide bond. The linkage decreased the concentration of perchlorate required to stabilize the alpha-helical structure by 30-fold. With the dimeric Mastoparan derivative, we measured the effects of several salts such as sodium trichloroacetate, sodium trifluoroacetate, and sodium chloride. The concentration of salts required to induce the conformational transition varied and the order of effectiveness of different salts was consistent with the electroselectivity series of anions toward anion-exchange resins, indicating that the anion binding to the positively charged amino groups is responsible for the transition. These results suggest that the salt-induced formation of the alpha-helical state of Mastoparan can be explained by a mechanism similar to that proposed for the salt-induced conformational transition of melittin.