Amylin, amide, rat是一种大鼠来源的酰胺化肽激素，具有调节血糖的活性。
Cas No.:124447-81-0
Sample solution is provided at 25 µL, 10mM.
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Amylin, amide, rat is a GABA uptake inhibitor selective for the BGT-1 (mGAT-2) transporter[1-2]. Amylin, amide, rat lowers blood glucose levels by inhibiting glucagon secretion and delaying gastric emptying, while also increasing satiety through central nervous system action to reduce food intake. Amylin, amide, rat and its analogs are utilized in research on diabetes and related metabolic disorders[3-4].
In vitro, HepG2 human liver cancer cells were treated with Amylin, amide, rat (1nM–1µM) for 10-45 minutes. Amylin, amide, rat dose-dependently stimulated adenylate cyclase activity in their cell membrane preparations[5]. Amylin, amide, rat (1nM–1µM) was applied to HEK293S and Cos 7 cells expressing human amylin receptors, and the cAMP response was measured. Amylin, amide, rat significantly activated the AMY1(a) and AMY3(a) receptors while enhancing cAMP production[6].
In vivo, Amylin, amide, rat (0.312-80.0µg) was administered to rats via intracerebroventricular injection. Amylin, amide, rat dose-dependently reduced their spontaneous motor activity, significantly increased body temperature, and decreased food intake in animals fasted for 22 hours[7]. In anesthetized male Sprague-Dawley rats, a single intravenous injection of Amylin, amide, rat (10-1000pmol/kg) elicited a significant pressor response at low doses (10-100pmol/kg), which appeared within 30-60 seconds and lasted for 15 minutes, while also increasing plasma renin activity. Higher doses (>1nmol/kg) induced a depressor response[8].
References:
[1] Bower RL, Hay DL. Amylin structure-function relationships and receptor pharmacology: implications for amylin mimetic drug development. Br J Pharmacol. 2016 Jun;173(12):1883-98.
[2] Gostynska SE, Karim JA, Ford BE, et al. Amylin receptor subunit interactions are modulated by agonists and determine signaling. Sci Signal. 2025 Aug 19;18(900):eadt8127.
[3] Harris PJ, Cooper ME, Hiranyachattada S, et al. Amylin stimulates proximal tubular sodium transport and cell proliferation in the rat kidney. Am J Physiol. 1997 Jan;272(1 Pt 2):F13-21.
[4] Vine W, Smith P, LaChappell R, et al. Effects of rat amylin on renal function in the rat. Horm Metab Res. 1998 Aug;30(8):518-22.
[5] Sheriff S, Fischer JE, Balasubramaniam A. Characterization of amylin binding sites in a human hepatoblastoma cell line. Peptides. 1992 Nov-Dec;13(6):1193-9.
[6] Gingell JJ, Burns ER, Hay DL. Activity of pramlintide, rat and human amylin but not Aβ1-42 at human amylin receptors. Endocrinology. 2014 Jan;155(1):21-6.
[7] Bouali SM, Wimalawansa SJ, Jolicoeur FB. In vivo central actions of rat amylin. Regul Pept. 1995 Apr 14;56(2-3):167-74.
[8] Haynes JM, Hodgson WC, Cooper ME. Rat amylin mediates a pressor response in the anaesthetised rat: implications for the association between hypertension and diabetes mellitus. Diabetologia. 1997 Mar;40(3):256-61.
Amylin, amide, rat是一种大鼠来源的酰胺化肽激素，具有调节血糖的活性[1-2]。Amylin, amide, rat可通过抑制胰高血糖素分泌和延缓胃排空来降低血糖水平，同时通过中枢作用增加饱腹感以减少食物摄入。Amylin, amide, rat及其类似物可用于糖尿病和相关代谢疾病的研究[3-4]。
在体外，Amylin, amide, rat（1nM–1μM）处理人肝癌细胞HepG2 10-45分钟。Amylin, amide, rat可以剂量依赖性地刺激其细胞膜制备物中腺苷酸环化酶的活性[5]。Amylin, amide, rat（1nM–1μM）处理表达人amylin受体的HEK293S和Cos 7细胞，随后测量cAMP响应。Amylin, amide, rat显著激活AMY1(a)和AMY3(a)受体，同时增强cAMP产生[6]。
在体内，Amylin, amide, rat（0.312-80.0μg）通过侧脑室注射给予大鼠，Amylin, amide, rat可剂量依赖性地降低其自发运动活动并显著升高体温，同时减少禁食22小时动物的食物摄入[7]。Amylin, amide, rat（10-1000pmol/kg；单次静脉注射）用于处理麻醉的雄性Sprague-Dawley大鼠。Amylin, amide, rat可在低剂量（10-100pmol/kg）时引发显著的升压反应，该效应在30-60秒内出现并持续15分钟，同时增加血浆肾素活性。高剂量（>1nmol/kg）则引起降压反应[8]。
| Cell experiment [1]: | |
Cell lines | Human hepatoblastoma cell line (HepG2) |
Preparation Method | HepG2 cells were cultured in Minimum Essential Medium (MEM) supplemented with 10% fetal bovine serum at 37°C in a humidified 5% CO₂ atmosphere. For adenylate cyclase and desensitization experiments, cell membrane preparations or intact cells were treated with Amylin, amide, rat (1nM-1μM) or rat CGRP. |
Reaction Conditions | 1nM-1μM; 10-45min. |
Applications | Amylin, amide, rat bound with high affinity (Kd=0.11nM) and specificity to distinct receptors on HepG2 cells. Amylin, amide, rat stimulated adenylate cyclase activity of HepG2 cell membranes in a dose-dependent manner, an effect significantly attenuated by the CGRP receptor antagonist hCGRP(8-37). |
| Animal experiment [2]: | |
Animal models | Male hooded rats |
Preparation Method | Rats were implanted with a guide cannula targeting the left lateral cerebro-ventricle under anesthesia. After a recovery period of at least 4 days, Amylin, amide, rat (0.312-80.0μg per rat) was administered via intracerebroventricular (i.c.v.) injection. A battery of neurobehavioral tests (spontaneous motor activity, catalepsy, muscular tone, body temperature, nociception) was performed immediately before and at intervals for 2 hours after injection. For food intake studies, separate groups of rats on a restricted feeding schedule were injected prior to their feeding period. |
Dosage form | 0.312-80.0μg per rat; i.c.v.; single injection. |
Applications | Intracerebroventricular administration of Amylin, amide, rat significantly and dose-dependently reduced spontaneous motor activity and markedly increased body temperature. Amylin, amide, rat also significantly reduced food consumption in 22-hour food-deprived animals. However, even at the highest dose (80.0μg), Amylin, amide, rat did not affect nociceptive response, induce catalepsy, or alter muscular tone. |
References: | |
| Cas No. | 124447-81-0 | SDF | |
| 别名 | Amylin (rat) | ||
| 分子式 | C167H272N52O53S2 | 分子量 | 3920.44 |
| 溶解度 | H2O : 100 mg/mL (25.51 mM; Need ultrasonic); DMSO : 50 mg/mL (12.75 mM; Need ultrasonic) | 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 | 255.1 μL | 1.2754 mL | 2.5507 mL |
| 5 mM | 51 μL | 255.1 μL | 510.1 μL |
| 10 mM | 25.5 μL | 127.5 μL | 255.1 μL |
| 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 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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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，
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2.
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