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| 1mg |
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| 5mg | |||
| Other Sizes |
| Targets |
Amylin (8-37), rat targets the amylin receptor (AMY), a G protein-coupled receptor belonging to the GPCR/G Protein pathway. The amylin receptor is a heterodimer composed of the calcitonin receptor core and receptor activity-modifying proteins (RAMPs). Amylin is a peptide hormone co-secreted with insulin from pancreatic beta-cells that regulates glucose homeostasis, gastric emptying, and satiety. As a truncated analog lacking the N-terminal region critical for full agonism, Amylin (8-37), rat acts as a weak antagonist at the amylin receptor. By blocking amylin receptor signaling, this peptide prevents amylin-induced inhibition of insulin-related glucose uptake and glycogen synthesis in skeletal muscle, making it a valuable tool for studying amylin physiology and its role in metabolic disorders such as type 2 diabetes and insulin resistance.
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| ln Vitro |
In both insulin-resistant and normal rats, amylin (8-37), or rat amylin-(8-37), modifies lipid metabolism and increases the action of insulin. Amylin (8–37) increased several measures of systemic and muscle insulin sensitivity (P<0.05) and decreased plasma insulin (P<0.001) in rats given saline and hGH injections. Amylin (8–37) reduced muscle triglycerides and total long-chain acyl-CoA in saline-treated rats, decreased basal plasma triglycerides and decreased plasma non-esterified fatty acids in both groups, and corrected hGH-induced hepatic insulin resistance (P < 0.05). Amylin (8–37) inhibits the inhibition of glycogen synthesis caused by amylin in isolated soleus muscle, but it has no effect when amylin is not present. Thus, 1) hGH infusion-induced insulin resistance is accompanied by hyperamylemia; 2) Amylin (8-37) consistently lowers basal insulin levels and increases systemic and muscle insulin sensitivity in both normal and hGH-induced insulin-resistant rats; and 3) Amylin (8-37) significantly alters the body's lipid metabolism [2].
In vitro, Amylin (8-37), rat enhances insulin action and alters lipid metabolism in normal and insulin-resistant rat models. The peptide reduces plasma insulin levels (P<0.001) and enhances several measures of whole-body and muscle insulin sensitivity (P<0.05) in both saline- and hGH-infused rats. In isolated soleus muscle, Amylin (8-37) blocks amylin-induced inhibition of glycogen synthesis but has no effect in the absence of amylin. The peptide corrects hGH-induced liver insulin resistance, increases basal plasma triglycerides, and lowers plasma nonesterified fatty acids in both treatment groups. These findings demonstrate that Amylin (8-37) can counteract amylin-mediated metabolic effects and improve insulin sensitivity in vitro. |
| ln Vivo |
In vivo, Amylin (8-37), rat has been shown to increase whole-body and muscle insulin sensitivity and consistently reduce basal insulin levels in normal and hGH-induced insulin-resistant rats. Administration of the peptide elicits significant alterations in lipid metabolism in vivo. Studies indicate that hyperamylinemia accompanies insulin resistance induced by hGH infusion, and Amylin (8-37) treatment can reverse some of these metabolic disturbances. The peptide's ability to improve insulin sensitivity and modulate lipid metabolism in animal models supports its utility as a research tool for investigating amylin's physiological roles and its contribution to insulin resistance and metabolic syndrome.
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| Enzyme Assay |
In vitro receptor binding assays for Amylin (8-37), rat involve measuring competitive binding affinity to the amylin receptor using radiolabeled amylin ligands. Membrane preparations from cells expressing the amylin receptor (e.g., CHO cells co-expressing the calcitonin receptor and RAMP components) are incubated with a radiolabeled amylin tracer (such as [¹2⁵I]-amylin) and varying concentrations of the test peptide. Bound and free radioligand are separated by filtration or centrifugation, and radioactivity is quantified by gamma counting. Binding affinity (Ki or IC50) is calculated from competition curves using non-linear regression analysis. Functional antagonism can be assessed by measuring inhibition of amylin-stimulated cAMP accumulation or calcium mobilization in receptor-expressing cells. Each concentration is typically tested in duplicate or triplicate with appropriate positive controls (e.g., unlabeled amylin) and vehicle controls.
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| Cell Assay |
In vitro cellular assays for Amylin (8-37), rat are performed using amylin receptor-expressing cell lines or primary cells such as isolated skeletal muscle preparations. For receptor signaling assays, cells expressing the amylin receptor are treated with a fixed concentration of amylin agonist and varying concentrations of the test peptide, and downstream signaling (e.g., cAMP accumulation, calcium flux) is measured. In isolated soleus muscle assays, muscles are incubated with amylin in the presence or absence of Amylin (8-37), and glycogen synthesis is measured by [14C]-glucose incorporation. For insulin sensitivity studies, cells or tissues are treated with insulin and the peptide, and glucose uptake is measured using radiolabeled 2-deoxyglucose or fluorescent glucose analogs. Cytotoxicity is assessed in parallel using standard viability assays to ensure observed effects are not due to cell death.
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| Animal Protocol |
In vivo animal studies for Amylin (8-37), rat are conducted using rodent models of insulin resistance and metabolic syndrome. Normal rats or hGH-induced insulin-resistant rats are administered the peptide via subcutaneous or intraperitoneal injection at various doses. Metabolic parameters including plasma insulin, glucose, triglycerides, and nonesterified fatty acids are measured at baseline and following treatment. Insulin sensitivity is assessed using hyperinsulinemic-euglycemic clamp techniques or insulin tolerance tests. Tissue samples (liver, muscle, adipose) are collected for analysis of glycogen content, lipid metabolism, and insulin signaling markers. Body weight and food intake are monitored throughout the study. Pharmacokinetic studies may assess peptide concentrations in plasma. Efficacy is expressed as changes in metabolic parameters and insulin sensitivity compared to vehicle-treated controls.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Amylin (8-37), rat are characteristic of a peptide therapeutic. The peptide has a molecular formula of C140H227N43O43 and a molecular weight of 3200.61 g/mol. It is soluble in water at 50 mg/mL with ultrasonic assistance. As a peptide, Amylin (8-37) is susceptible to proteolytic degradation and has a relatively short half-life in circulation. The peptide is typically administered by injection (subcutaneous, intraperitoneal, or intravenous) due to poor oral bioavailability. Its stability in solution is limited, and fresh solutions are typically prepared for experiments. Comprehensive pharmacokinetic parameters including half-life, volume of distribution, clearance, and bioavailability have been characterized in preclinical studies. The peptide's pharmacokinetic profile supports its use as a research tool for acute metabolic studies.
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| Toxicity/Toxicokinetics |
Amylin (8-37), rat is intended for laboratory research use only and has not undergone comprehensive clinical toxicology testing. As a truncated peptide derived from a naturally occurring hormone, the compound is generally well-tolerated in preclinical studies at research-use concentrations. Standard in vitro cytotoxicity assays in cell lines are typically performed alongside efficacy studies to rule out nonspecific toxicity. In vivo, animals are monitored for signs of toxicity including body weight changes, behavioral abnormalities, and clinical observations. Comprehensive toxicological characterization including genotoxicity and repeated-dose toxicity studies has not been extensively reported for Amylin (8-37), as the compound is primarily used as a research tool rather than a therapeutic candidate. The peptide is not approved for human use and is strictly intended for research purposes.
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| References |
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| Additional Infomation |
Amylin (8-37), rat is a truncated synthetic peptide analog of native rat amylin that acts as a weak antagonist at the amylin receptor (AMY). It selectively inhibits insulin-related glucose uptake and glycogen deposition in muscle tissue. The peptide has the sequence ATQRLANFLVRSSNNLGPVLPPTNVGSNTY-NH2 and a molecular weight of 3200.61 g/mol. Amylin (8-37) enhances insulin action and alters lipid metabolism in normal and insulin-resistant rats. The peptide is widely used in metabolic research to study amylin's role in insulin resistance, glucose metabolism, and lipid regulation. Amylin (8-37), rat has not entered clinical trials and has not received regulatory approval for any indication. It is available from research chemical suppliers for non-clinical research purposes only.
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| Molecular Formula |
C140H227N43O43
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|---|---|
| Molecular Weight |
3200.56000
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| Exact Mass |
3198.69
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| CAS # |
138398-61-5
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| PubChem CID |
102601646
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| Appearance |
White to off-white solid powder
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| LogP |
-13
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| Hydrogen Bond Donor Count |
47
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| Hydrogen Bond Acceptor Count |
46
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| Rotatable Bond Count |
100
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| Heavy Atom Count |
226
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| Complexity |
7650
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| Defined Atom Stereocenter Count |
31
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| SMILES |
C[C@H]([C@@H](C(=O)N[C@@H](CC(=O)N)C(=O)N[C@@H](C(C)C)C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CC(=O)N)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC1=CC=C(C=C1)O)C(=O)N)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]3CCCN3C(=O)[C@H](CC(C)C)NC(=O)[C@H](C(C)C)NC(=O)[C@@H]4CCCN4C(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)N)NC(=O)[C@H](CC(=O)N)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC5=CC=CC=C5)NC(=O)[C@H](CC(=O)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](C)N)O
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| InChi Key |
KXIRMGRGEHRNNC-ANJGTFPLSA-N
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| InChi Code |
InChI=1S/C140H227N43O43/c1-62(2)46-81(114(202)156-58-104(198)181-43-25-32-94(181)129(217)177-107(68(13)14)133(221)172-90(49-65(7)8)137(225)183-45-27-34-96(183)138(226)182-44-26-33-95(182)130(218)180-110(73(19)189)136(224)171-89(56-102(147)196)124(212)175-105(66(9)10)131(219)155-57-103(197)158-91(59-184)126(214)170-88(55-101(146)195)125(213)179-109(72(18)188)135(223)162-80(111(148)199)50-75-35-37-76(190)38-36-75)164-121(209)86(53-99(144)193)168-122(210)87(54-100(145)194)169-127(215)92(60-185)174-128(216)93(61-186)173-116(204)78(31-24-42-154-140(151)152)160-132(220)106(67(11)12)176-123(211)83(48-64(5)6)166-119(207)84(51-74-28-21-20-22-29-74)167-120(208)85(52-98(143)192)163-113(201)70(16)157-118(206)82(47-63(3)4)165-115(203)77(30-23-41-153-139(149)150)159-117(205)79(39-40-97(142)191)161-134(222)108(71(17)187)178-112(200)69(15)141/h20-22,28-29,35-38,62-73,77-96,105-110,184-190H,23-27,30-34,39-61,141H2,1-19H3,(H2,142,191)(H2,143,192)(H2,144,193)(H2,145,194)(H2,146,195)(H2,147,196)(H2,148,199)(H,155,219)(H,156,202)(H,157,206)(H,158,197)(H,159,205)(H,160,220)(H,161,222)(H,162,223)(H,163,201)(H,164,209)(H,165,203)(H,166,207)(H,167,208)(H,168,210)(H,169,215)(H,170,214)(H,171,224)(H,172,221)(H,173,204)(H,174,216)(H,175,212)(H,176,211)(H,177,217)(H,178,200)(H,179,213)(H,180,218)(H4,149,150,153)(H4,151,152,154)/t69-,70-,71+,72+,73+,77-,78-,79-,80-,81-,82-,83-,84-,85-,86-,87-,88-,89-,90-,91-,92-,93-,94-,95-,96-,105-,106-,107-,108-,109-,110-/m0/s1
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| Chemical Name |
(2S)-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-4-amino-1-[[(2S)-1-[[2-[(2S)-2-[[(2S)-1-[[(2S)-1-[(2S)-2-[(2S)-2-[[(2S,3R)-1-[[(2S)-4-amino-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-4-amino-1-[[(2S,3R)-1-[[(2S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]carbamoyl]pyrrolidine-1-carbonyl]pyrrolidin-1-yl]-4-methyl-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]carbamoyl]pyrrolidin-1-yl]-2-oxoethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]-2-[[(2S,3R)-2-[[(2S)-2-aminopropanoyl]amino]-3-hydroxybutanoyl]amino]pentanediamide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : ~50 mg/mL (~15.62 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.3124 mL | 1.5622 mL | 3.1245 mL | |
| 5 mM | 0.0625 mL | 0.3124 mL | 0.6249 mL | |
| 10 mM | 0.0312 mL | 0.1562 mL | 0.3124 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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