| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg | |||
| Other Sizes |
| Targets |
GIP receptor (antagonist). GIP (3-42), human is an antagonist of the GIP receptor. It binds to the receptor without activating it, thereby blocking the actions of endogenous GIP, including insulin secretion and metabolic regulation.
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|---|---|
| ln Vitro |
Dipeptidyl peptidase IV (DPP IV) quickly breaks down the incretin hormone GIP in the bloodstream to produce the N-terminally truncated peptide GIP(3-42)[1].
At high concentrations, GIP(3-42) acts as a low-potency antagonist of the GIP receptor, weakly antagonizing cAMP accumulation and insulin output in vitro with an IC50 of 22 nM. It is an antagonist of the GIP receptor that modulates insulin secretion and GIP metabolism in vivo. |
| ln Vivo |
GIP (3-42), human acts as a GIP receptor antagonist in vivo, moderating the insulin-secreting and metabolic actions of GIP. Evidence indicates that the major degradation product of GIP, GIP(3-42), is a GIP receptor antagonist, and it does not produce physiological antagonism in vivo at low concentrations, but at higher concentrations, it can modulate GIP effects.
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| Enzyme Assay |
Cell-free GIP receptor binding assays are performed using membranes from cells expressing the human GIP receptor. Membranes are incubated with a radiolabeled GIP ligand and increasing concentrations of GIP (3-42), human. The amount of bound radioactivity is measured to determine binding affinity and antagonist potency (IC50 = 22 nM).
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| Cell Assay |
Cells expressing the human GIP receptor are loaded with a cAMP detection kit (HTRF). Cells are pre-incubated with GIP (3-42) at various concentrations (0.1-1000 nM) for 10-15 min, then stimulated with native GIP (1-10 nM). Antagonism is assessed by measuring the reduction in GIP-stimulated cAMP accumulation. IC50 = 22 nM. Insulin secretion can be measured in beta-cell lines.
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| Animal Protocol |
For in vivo studies, GIP (3-42) is administered to mice or rats via intraperitoneal injection prior to glucose challenge or GIP administration. Glucose tolerance tests are performed, and plasma insulin and glucose levels are measured. The in vivo antagonism of GIP (3-42) is assessed by its ability to block GIP-induced insulin secretion. It can be used to study the physiological role of GIP.
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| ADME/Pharmacokinetics |
No specific PK data are reported for GIP (3-42), human. As a peptide fragment of GIP, it is not orally bioavailable and has a short half-life due to rapid degradation by peptidases. For in vivo studies, it is typically administered by injection. Molecular weight: 4353.9. CAS 1802086-25-4. Solubility: water (≥10 mg/mL).
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| Toxicity/Toxicokinetics |
No specific toxicity data are reported. As a peptide fragment that is an endogenous degradation product of GIP, it is not expected to have significant toxicity at research doses. Comprehensive toxicological assessments have not been performed. The compound is for research use only and is not a therapeutic agent.
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| References |
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| Additional Infomation |
Other information: GIP (3-42), human (CAS 1802086-25-4) is a research-grade peptide, not FDA-approved. It is a GIP receptor antagonist that represents the major degradation product of GIP formed by DPP-4. It is a valuable tool for studying incretin biology and the role of GIP in glucose homeostasis. For research use only.
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| Molecular Formula |
C214H324N58O63S
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|---|---|
| Molecular Weight |
4749.40
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| Exact Mass |
4390.186
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| CAS # |
1802086-25-4
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| PubChem CID |
171397201
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| Appearance |
White to off-white solid powder
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| LogP |
-22.4
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| Hydrogen Bond Donor Count |
61
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| Hydrogen Bond Acceptor Count |
66
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| Rotatable Bond Count |
150
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| Heavy Atom Count |
311
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| Complexity |
10700
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| Defined Atom Stereocenter Count |
39
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| SMILES |
CC[C@H](C)[C@@H](C(=O)N[C@@H](CC1=CNC=N1)C(=O)N[C@@H](CCC(=O)N)C(=O)N[C@@H](CCC(=O)N)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CC2=CC=CC=C2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(=O)N)C(=O)N[C@@H](CC3=CNC4=CC=CC=C43)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)N)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(=O)N)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CC5=CNC6=CC=CC=C65)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC7=CNC=N7)C(=O)N[C@@H](CC(=O)N)C=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@H](C)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](CC8=CC=C(C=C8)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CC9=CC=CC=C9)NC(=O)[C@H]([C@@H](C)O)NC(=O)CNC(=O)[C@H](CCC(=O)O)N
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| InChi Key |
QYLDDJIZEWSFPS-YUZGIZTPSA-N
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| InChi Code |
InChI=1S/C199H298N54O57S/c1-17-102(10)162(253-194(305)147(96-256)247-181(292)133(76-110-53-55-116(258)56-54-110)234-189(300)145(87-160(275)276)243-193(304)146(95-255)248-198(309)164(104(12)19-3)252-192(303)135(75-109-42-24-21-25-43-109)244-199(310)165(107(15)257)249-155(266)93-216-168(279)119(205)57-64-156(267)268)196(307)221-106(14)167(278)225-130(65-71-311-16)176(287)241-142(84-157(269)270)187(298)229-126(52-34-39-70-204)177(288)251-163(103(11)18-2)197(308)245-139(80-114-91-213-98-219-114)184(295)231-128(59-62-149(207)260)174(285)230-129(60-63-150(208)261)175(286)240-143(85-158(271)272)188(299)235-134(74-108-40-22-20-23-41-108)191(302)250-161(101(8)9)195(306)246-141(83-153(211)264)186(297)236-137(78-112-89-215-121-47-29-27-45-118(112)121)183(294)233-132(73-100(6)7)180(291)232-131(72-99(4)5)178(289)220-105(13)166(277)224-127(58-61-148(206)259)173(284)226-122(48-30-35-66-200)169(280)217-92-154(265)223-123(49-31-36-67-201)170(281)227-124(50-32-37-68-202)172(283)239-140(82-152(210)263)185(296)242-144(86-159(273)274)190(301)237-136(77-111-88-214-120-46-28-26-44-117(111)120)182(293)228-125(51-33-38-69-203)171(282)238-138(79-113-90-212-97-218-113)179(290)222-115(94-254)81-151(209)262/h20-29,40-47,53-56,88-91,94,97-107,115,119,122-147,161-165,214-215,255-258H,17-19,30-39,48-52,57-87,92-93,95-96,200-205H2,1-16H3,(H2,206,259)(H2,207,260)(H2,208,261)(H2,209,262)(H2,210,263)(H2,211,264)(H,212,218)(H,213,219)(H,216,279)(H,217,280)(H,220,289)(H,221,307)(H,222,290)(H,223,265)(H,224,277)(H,225,278)(H,226,284)(H,227,281)(H,228,293)(H,229,298)(H,230,285)(H,231,295)(H,232,291)(H,233,294)(H,234,300)(H,235,299)(H,236,297)(H,237,301)(H,238,282)(H,239,283)(H,240,286)(H,241,287)(H,242,296)(H,243,304)(H,244,310)(H,245,308)(H,246,306)(H,247,292)(H,248,309)(H,249,266)(H,250,302)(H,251,288)(H,252,303)(H,253,305)(H,267,268)(H,269,270)(H,271,272)(H,273,274)(H,275,276)/t102-,103-,104-,105-,106-,107+,115-,119-,122-,123-,124-,125-,126-,127-,128-,129-,130-,131-,132-,133-,134-,135-,136-,137-,138-,139-,140-,141-,142-,143-,144-,145-,146-,147-,161-,162-,163-,164-,165-/m0/s1
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| Chemical Name |
(4S)-4-amino-5-[[2-[[(2S,3R)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-6-amino-1-[[2-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-4-amino-1,4-dioxobutan-2-yl]amino]-3-(1H-imidazol-4-yl)-1-oxopropan-2-yl]amino]-1-oxohexan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-2-oxoethyl]amino]-1-oxohexan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-3-(1H-imidazol-4-yl)-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-2-oxoethyl]amino]-5-oxopentanoic acid
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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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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) |
DMSO: 100 mg/mL (21.06 mM)
H2O: 50 mg/mL (10.53 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 10 mg/mL (2.11 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.2106 mL | 1.0528 mL | 2.1055 mL | |
| 5 mM | 0.0421 mL | 0.2106 mL | 0.4211 mL | |
| 10 mM | 0.0211 mL | 0.1053 mL | 0.2106 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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