| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
GPR39 (G protein-coupled receptor 39). Rat obestatin shows high affinity binding to GPR39 expressing cells (Kd ≈ 1 nM).
Obestatin is an endogenous ligand of the G-protein coupled receptor 39 (GPR39). It binds to GPR39 with high affinity (Kd ≈ 1 nM). GPR39 is an orphan GPCR that is encoded by the ghrelin gene and is involved in the regulation of appetite, gastrointestinal motility, and energy homeostasis. |
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| ln Vitro |
Obestatin antagonizes ghrelin-induced contraction in isolated jejunum muscle strips, effectively blocking the stimulatory effect of ghrelin on gastrointestinal motility. It also shows activity in cell-based assays such as stimulating cAMP production in GPR39-expressing cells.
In vitro, obestatin antagonizes ghrelin-induced contraction in isolated jejunum muscle strips, effectively blocking the stimulatory effect of ghrelin on gastrointestinal motility. It stimulates cAMP production in CHO and HEK293 cells overexpressing human GPR39. The peptide also exhibits anti-inflammatory, anti-myocardial infarction, and antioxidant activities. |
| ln Vivo |
In animal models, obestatin suppresses food intake in a dose-dependent manner, reduces body weight gain, and inhibits jejunal contraction and gastric emptying. These effects are contrary to the appetite-stimulating effects of ghrelin.
In vivo, obestatin suppresses food intake in a dose-dependent manner, reduces body weight gain, and inhibits jejunal contraction and gastric emptying in rodent models. These effects are contrary to the appetite-stimulating effects of ghrelin. The peptide is typically administered via intraperitoneal (IP) injection in doses ranging from 12.5 to 1000 nmol/kg. |
| Enzyme Assay |
The binding affinity of Obestatin(rat) to GPR39 is determined via radioligand binding assays. Membranes from cells overexpressing GPR39 are incubated with iodinated obestatin and varying concentrations of unlabeled peptide, allowing calculation of the dissociation constant (Kd ≈ 1 nM).
Receptor binding assays for obestatin utilize radioligand binding with membranes from cells overexpressing GPR39. Membranes are incubated with iodinated obestatin and varying concentrations of unlabeled peptide, allowing calculation of the dissociation constant (Kd ≈ 1 nM). |
| Cell Assay |
The functional activity of obestatin is often measured using cAMP accumulation assays in CHO or HEK293 cell lines stably or transiently expressing the human GPR39 receptor. Cells are stimulated with the peptide, and the resulting intracellular cAMP levels are quantified to confirm receptor activation.
Functional activity of obestatin is measured using cAMP accumulation assays in CHO or HEK293 cell lines stably or transiently expressing human GPR39. Cells are stimulated with the peptide, and intracellular cAMP levels are quantified to confirm receptor activation. |
| Animal Protocol |
The peptide is typically administered via intraperitoneal (IP) injection in rodent models to study its effects on feeding behavior. Doses in the range of 12.5-1000 nmol/kg are commonly used to suppress food intake. For specific studies, it is dissolved in sterile saline for injection.
Obestatin is typically administered via intraperitoneal (IP) injection in rodent models to study its effects on feeding behavior. Doses in the range of 12.5-1000 nmol/kg are commonly used to suppress food intake. For specific studies, the peptide is dissolved in sterile saline for injection. |
| ADME/Pharmacokinetics |
Obestatin is a peptide that is rapidly degraded in vivo. It is derived from the preproghrelin protein and is found in the stomach. It is susceptible to proteolytic cleavage by enzymes in the serum and gastrointestinal tract, which contributes to its short half-life in circulation.
Obestatin is a peptide that is rapidly degraded in vivo. It is derived from the preproghrelin protein and is found in the stomach. It is susceptible to proteolytic cleavage by enzymes in the serum and gastrointestinal tract, contributing to its short half-life in circulation. |
| Toxicity/Toxicokinetics |
Toxicity data for obestatin are limited. Peptide research compounds are generally considered to have low toxicity at pharmacological doses. Standard laboratory safety practices should be followed when handling this compound.
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| References | |
| Additional Infomation |
Obestatin (rat) is a research-use peptide not approved for therapeutic applications. It is a synthetic form of the endogenous peptide hormone produced in the rat stomach. The compound has a molecular formula of C114H1₇4N34O31 and a molecular weight of 2516.81. It is structurally related to ghrelin and is used to study appetite regulation and energy balance.
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| Molecular Formula |
C114H174N34O31
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|---|---|
| Molecular Weight |
2516.81000
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| Exact Mass |
2515.31
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| CAS # |
869705-22-6
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| Related CAS # |
Obestatin(rat) TFA;1312186-27-8
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| PubChem CID |
71311910
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| Sequence |
H-Phe-Asn-Ala-Pro-Phe-Asp-Val-Gly-Ile-Lys-Leu-Ser-Gly-Ala-Gln-Tyr-Gln-Gln-His-Gly-Arg-Ala-Leu-NH2
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| SequenceShortening |
FNAPFDVGIKLSGAQYQQHGRAL
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| Appearance |
White to off-white solid powder
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| LogP |
2.889
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| Hydrogen Bond Donor Count |
35
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| Hydrogen Bond Acceptor Count |
35
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| Rotatable Bond Count |
82
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| Heavy Atom Count |
179
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| Complexity |
5670
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| Defined Atom Stereocenter Count |
21
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| SMILES |
CC[C@H](C)[C@@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)N)C(=O)N[C@@H](CC1=CC=C(C=C1)O)C(=O)N[C@@H](CCC(=O)N)C(=O)N[C@@H](CCC(=O)N)C(=O)N[C@@H](CC2=CNC=N2)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)N)NC(=O)CNC(=O)[C@H](C(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC3=CC=CC=C3)NC(=O)[C@@H]4CCCN4C(=O)[C@H](C)NC(=O)[C@H](CC(=O)N)NC(=O)[C@H](CC5=CC=CC=C5)N
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| InChi Key |
OJSXICLEROKMBP-FFUDWAICSA-N
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| InChi Code |
InChI=1S/C114H174N34O31/c1-12-60(8)93(146-90(157)54-128-111(177)92(59(6)7)147-109(175)81(50-91(158)159)143-108(174)78(46-65-25-17-14-18-26-65)144-110(176)83-29-22-42-148(83)113(179)63(11)132-105(171)80(49-87(120)154)139-97(163)69(116)45-64-23-15-13-16-24-64)112(178)137-71(27-19-20-40-115)101(167)140-76(44-58(4)5)106(172)145-82(55-149)99(165)127-52-88(155)130-61(9)95(161)134-72(34-37-84(117)151)103(169)141-77(47-66-30-32-68(150)33-31-66)107(173)136-73(35-38-85(118)152)102(168)135-74(36-39-86(119)153)104(170)142-79(48-67-51-124-56-129-67)98(164)126-53-89(156)133-70(28-21-41-125-114(122)123)100(166)131-62(10)96(162)138-75(94(121)160)43-57(2)3/h13-18,23-26,30-33,51,56-63,69-83,92-93,149-150H,12,19-22,27-29,34-50,52-55,115-116H2,1-11H3,(H2,117,151)(H2,118,152)(H2,119,153)(H2,120,154)(H2,121,160)(H,124,129)(H,126,164)(H,127,165)(H,128,177)(H,130,155)(H,131,166)(H,132,171)(H,133,156)(H,134,161)(H,135,168)(H,136,173)(H,137,178)(H,138,162)(H,139,163)(H,140,167)(H,141,169)(H,142,170)(H,143,174)(H,144,176)(H,145,172)(H,146,157)(H,147,175)(H,158,159)(H4,122,123,125)/t60-,61-,62-,63-,69-,70-,71-,72-,73-,74-,75-,76-,77-,78-,79-,80-,81-,82-,83-,92-,93-/m0/s1
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| Chemical Name |
(3S)-4-[[(2S)-1-[[2-[[(2S,3S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-5-amino-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-3-(1H-imidazol-4-yl)-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-amino-3-phenylpropanoyl]amino]-4-oxobutanoyl]amino]propanoyl]pyrrolidine-2-carbonyl]amino]-3-phenylpropanoyl]amino]-4-oxobutanoic acid
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| Synonyms |
Obestatin (rat); 869705-22-6; Obestatin, rat, mouse; orb1296338; Obestatin mouse, rat, synthetic;
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 0.3973 mL | 1.9866 mL | 3.9733 mL | |
| 5 mM | 0.0795 mL | 0.3973 mL | 0.7947 mL | |
| 10 mM | 0.0397 mL | 0.1987 mL | 0.3973 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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