Hemokinin 1 (mouse)
目录号 : GC13239
Hemokinin 1 (mouse) 是一种选择性的神经激肽-1 受体激动剂，对人 NK1 受体和人 NK2 受体的 Ki 分别为 0.175 nM 和 560 nM。
Cas No.:208041-90-1
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
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- Purity: >98.00%
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Animal experiment: | Male albino Wistar Rats weighing 400-450 g are used throughout the study. On the day of the experiment, rats are anaesthetized with urethane (1.2 g/kg, s.c.). Following tracheotomy and placement of a tracheal cannula (PE 205), the left jugular vein is cannulated (PE50) for SP or Hemokinin 1 (mouse) administrations. The body temperature is maintained constant (36.5±0.5°C) by a thermoregulated heating lamp. About 1 h elapsed between the animal set-up and the start of the experiments, thereafter each animal receive atropine (1.4 μmol/kg i.v. as bolus followed by infusion of 1.4 μM in a volume of 300 μL/h) and 10 min later the vehicle (saline) and increasing doses (0.5 log units) of SP or Hemokinin 1 (mouse) (0.01, 0.03, 0.1, 0.3, 1, 3, 10, 30, and 100 nmol/kg); the first five doses are administered at 20 min intervals, whereas 30 min elapsed between each of the last four doses. Atropine pretreatment is performed in order to minimize the influence of cholinergic secretory reflexes in response to the placement of the cotton swab in the rat's oral cavity for the measurement of salivary secretion induced by SP or Hemokinin 1 (mouse). |
References: [1]. Francesca Bellucci, et al. Pharmacological profile of the novel mammalian tachykinin, hemokinin 1. Br J Pharmacol. 2002 Jan; 135(1): 266-274 | |
Hemokinin 1 (mouse) is a selective agonist of neurokinin-1 receptor, with Ki of 0.175 nM and 560 nM for human NK1 receptor and human NK2 receptor, respectively.
Hemokinin 1 (mouse) (1 nM-3 μM) produces concentration-dependent contraction of RUB averaging 66±3% (n=6) of the maximal contraction produced by KCl (80 mM). Hemokinin 1 (mouse) (10 nM-10 μM) induces a quickly-developing contractile responses of GPI, as does the tachykinin NK3 receptor selective agonist senktide or neurokinin B (NKB). Hemokinin 1 (mouse) induces full agonist responses but with a 500 fold lower potency as compared to NKB[1].
Hemokinin 1 (mouse) (0.01-100 nmol/kg i.v., n=10) induces a dose-related hypotension that is maximal at the dose of 10 nmol/kg. For systolic blood pressure (SBP), the ED50 value is 0.2 nmol/kg (0.1-0.4 nmol/kg) for Hemokinin 1 (mouse). For diastolic blood pressure (DBP), the ED50 value is 0.1 nmol/kg (0.07-0.2 nmol/kg) for Hemokinin 1 (mouse). Hemokinin 1 (mouse) (0.1-100 nmol/kg, i.v.) induces a dose-related salivary secretion in atropine-pretreated rats[1].
Reference:
[1]. Francesca Bellucci, et al. Pharmacological profile of the novel mammalian tachykinin, hemokinin 1. Br J Pharmacol. 2002 Jan; 135(1): 266-274
| Cas No. | 208041-90-1 | SDF | |
| 化学名 | (S,Z)-2-((Z)-((6S,7Z,9S,10Z,12S,13Z,15S,16Z,18S)-1,6-diamino-12,18-bis(3-guanidinopropyl)-7,10,13,16,19-pentahydroxy-15-((R)-1-hydroxyethyl)-9-(hydroxymethyl)-1-imino-2,8,11,14,17-pentaazanonadeca-7,10,13,16-tetraen-19-ylidene)amino)-N'1-((5S,6Z,8S,9Z,12Z | ||
| Canonical SMILES | CC(C[C@@](/N=C(O)/C/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](N)([H])CCCNC(N)=N)([H])CO)([H])CCCNC(N)=N)([H])[C@@](O)([H])C)([H])CCCNC(N)=N)([H])CCC(O)=N)([H])CC1=CC=CC=C1)([H])CC2=CC=C(O)C=C2)( | ||
| 分子式 | C61H100N22O15S | 分子量 | 1413.65 |
| 溶解度 | Soluble to 2 mg/ml in sterile water | 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 | 0.7074 mL | 3.5369 mL | 7.0739 mL |
| 5 mM | 0.1415 mL | 0.7074 mL | 1.4148 mL |
| 10 mM | 0.0707 mL | 0.3537 mL | 0.7074 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。
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