HS-014 (trifluoroacetate salt)
(Synonyms: Cyclic [Ac-Cys11, D-Nal14, Cys18, Asp-NH2]-β-MSH(11-22)) 目录号 : GC92103HS-014 (trifluoroacetate salt)是黑素皮质素受体4mc4r的拮抗剂；Ki = 3.16 nM。
Sample solution is provided at 25 µL, 10mM.
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HS-014 is an antagonist of melanocortin receptor 4 (MC4R; Ki = 3.16 nM).1 It is selective for MC4R over MC1R, MC3R, and MC5R (Kis = 108, 54.4, and 694 nM, respectively). HS-014 inhibits cAMP accumulation induced by α-melanocyte-stimulating hormone (α-MSH) in COS-1 cells expressing MC4R in a concentration-dependent manner. It increases food intake in free-feeding rats when administered intracerebroventricularly at doses of 1 or 3 nmol/animal.2 Intracerebroventricular administration of HS-014 (0.008 ng/animal) increases the latency to tail withdrawal in the tail-flick test, as well as inhibits morphine withdrawal-induced decreases in the latency to tail withdrawal in the tail-flick test, in rats.3 It reduces immobility time in the forced swim test, as well as increases time in the open area and reduces the number of droppings in an open field test, in rats when administered at a dose of 100 ?g/animal.4
References:
[1]. Schi?th, H.B., Mutulis, F., Muceniece, R., et al.Discovery of novel melanocortin4 receptor selective MSH analoguesBr. J. Pharmacol.124(1)75-82(1998).
[2]. Kask, A., R?go, L., Mutulis, F., et al.Selective antagonist for the melanocortin 4 receptor (HS014) increases food intake in free-feeding ratsBiochem. Biophys. Res. Commun.245(1)90-93(1998).
[3]. Kalange, A.S., Kokare, D.M., Singru, P.S., et al.Central administration of selective melanocortin 4 receptor antagonist HS014 prevents morphine tolerance and withdrawal hyperalgesiaBrain Res.118110-20(2007).
[4]. Serova, L.I., Laukova, M., Alaluf, L.G., et al.Intranasal infusion of melanocortin receptor four (MC4R) antagonist to rats ameliorates development of depression and anxiety related symptoms induced by single prolonged stressBehav. Brain Res.250139-147(2013).
| Cas No. | SDF | ||
| 别名 | Cyclic [Ac-Cys11, D-Nal14, Cys18, Asp-NH2]-β-MSH(11-22) | ||
| 化学名 | cyclic (1→8)-disulfide N-acetyl-L-cysteinyl-L-α-glutamyl-L-histidyl-3-(2-naphthalenyl)-D-alanyl-L-arginyl-L-tryptophylglycyl-L-cysteinyl-L-prolyl-L-prolyl-L-lysyl-L-α-asparagine, trifluoroacetate salt | ||
| Canonical SMILES | O=C([C@@H](NC([C@H](NC([C@@H](NC([C@@H](NC([C@H](CSSC[C@H](NC(CNC1=O)=O)C(N2[C@@H](CCC2)C(N3[C@@H](CCC3)C(N[C@@H](CCCCN)C(N[C@H](C(N)=O)CC(O)=O)=O)=O)=O)=O)NC(C)=O)=O)CCC(O)=O)=O)CC4=CN=CN4)=O)CC5=CC6=C(C=CC=C6)C=C5)=O)CCCNC(N)=N)N[C@H]1CC7=CNC8=CC=CC=C78.O=C(O)C(F)(F)F | ||
| 分子式 | C71H94N20O17S2 ? XCF3COOH | 分子量 | 1563.8 |
| 溶解度 | DMSO: Soluble: ≥10 mg/ml,PBS (pH 7.2): Soluble: ≥10 mg/ml | 储存条件 | -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 | 0.6395 mL | 3.1973 mL | 6.3947 mL |
| 5 mM | 0.1279 mL | 0.6395 mL | 1.2789 mL |
| 10 mM | 0.0639 mL | 0.3197 mL | 0.6395 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。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet