| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
The receptor target of obestatin has been a subject of significant controversy. In 2005, Zhang et al. first reported that obestatin is the endogenous ligand for the orphan G protein-coupled receptor GPR39. However, multiple subsequent independent studies failed to replicate this finding: Chartrel and colleagues (2007) demonstrated that ¹²⁵I-labeled obestatin does not bind to GPR39, and observed no effects of obestatin on GPR39-transfected cells in various functional assays including cyclic AMP production, calcium mobilization, and receptor internalization. Therefore, the current consensus is that GPR39 is not the physiological receptor for obestatin, and its true target remains to be identified.
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|---|---|
| ln Vitro |
Obestatin exhibits various biological activities at the cellular level in vitro. In porcine ovarian granulosa cell models, obestatin (1-100 ng/mL) significantly stimulates the expression of proliferation-associated proteins PCNA, cyclin B1, and MAPK, while simultaneously increasing the percentage of cells containing apoptotic markers p53, Caspase 3, and Bax, indicating that it can stimulate both cell proliferation and apoptosis. Regarding hormone secretion, obestatin at 10 and 100 ng/mL promotes progesteron
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| ln Vivo |
The in vivo activity of obestatin remains highly controversial. Early studies (2005) reported that intraperitoneal administration of obestatin suppressed food intake and reduced body weight gain in rats. However, multiple subsequent independent studies failed to validate these findings: In ghrelin knockout mice, peripheral administration of obestatin had no significant effect on 6-hour cumulative food intake or gastric emptying, suggesting that endogenous ghrelin does not mask the effect of obestatin. Additionally, obestatin (1 μmol/kg) reduced glucose excursions (64-77%) and insulin responses (39-41%), but these effects were accompanied by 43-53% reductions in food intake, and when feeding changes were excluded, obestatin had no direct effects on glucose homeostasis or insulin secretion.
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| Enzyme Assay |
Receptor binding assays for obestatin can be performed using radioligand binding analysis. Briefly, membrane homogenates from cells expressing the candidate receptor (e.g., GPR39) are incubated with ¹²⁵I-labeled obestatin (tracer) in binding buffer, along with various concentrations of unlabeled obestatin for competition binding. After incubation at room temperature for 60-90 minutes, the reaction is terminated by rapid vacuum filtration, and filters are washed with ice-cold buffer to remove unbound tracer. After drying, retained radioactivity on filters is measured using a gamma counter to calculate specific binding percentage and IC₅₀ values. Negative results should be validated using multiple functional assays (e.g., cAMP accumulation, calcium mobilization, receptor internalization).
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| Cell Assay |
Exponentially growing porcine ovarian granulosa cells are seeded at appropriate densities (typically 1-5×10⁴/well) into 24-well or 96-well culture plates. After attachment in DMEM/F12 medium containing 10% fetal bovine serum, cells are synchronized by replacing with serum-free medium for 12-24 hours. Various concentrations of obestatin (0, 1, 10, 100 ng/mL) are added and incubated for 24-48 hours. Expression of proliferation-associated proteins (PCNA, cyclin B1, MAPK) and apoptotic markers (p53, Caspase 3, Bax) is detected using immunocytochemistry and Western blotting. Cell culture supernatants are collected for determination of progesterone, testosterone, and estradiol secretion by enzyme immunoassay.
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| Animal Protocol |
Six-to-eight-week-old male wild-type (ghrelin⁺/⁺) or ghrelin knockout (ghrelin⁻/⁻) mice are used. Mice are fasted overnight (16-18 hours) prior to experiments. Obestatin is prepared in saline and administered intraperitoneally at doses of 1 μmol/kg or 300 μg/kg, with cumulative food intake monitored for 0-6 hours post-administration. Gastric emptying can be measured using the ¹⁴C-octanoic acid breath test: after intragastric administration of a test meal containing ¹⁴C-labeled octanoic acid, breath samples are collected at specified time intervals, and ¹⁴CO₂ excretion rates are measured by liquid scintillation counting to calculate gastric emptying half-life. Each experimental group typically contains 8-12 animals.
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| ADME/Pharmacokinetics |
As a peptide molecule, the pharmacokinetic profile of obestatin is characteristic of typical peptide drugs. To date, there are no published systematic pharmacokinetic studies of obestatin in animals, including parameters such as plasma half-life, bioavailability, volume of distribution, metabolic pathways, and excretion routes. As a peptide, obestatin has extremely low oral bioavailability and is typically administered via injection routes (intraperitoneal, subcutaneous, or intravenous). The TFA salt form is intended to improve peptide stability and solubility for experimental manipulation.
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| Toxicity/Toxicokinetics |
Toxicological data on obestatin are currently very limited. In published in vivo studies, obestatin at routine experimental doses (e.g., 1 μmol/kg intraperitoneal injection in mice) has not been reported to cause obvious acute toxicity reactions or behavioral abnormalities. Body weight and general condition of study animals remained normal during the experimental period. Due to the ongoing controversy surrounding the physiological function and mechanism of action of obestatin, and because it has not yet entered human clinical trials, toxicological safety data including long-term toxicity, genotoxicity, reproductive toxicity, and carcinogenicity are completely absent. Relevant products are explicitly stated for research use only and are not for human use.
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| References |
[1]. https://pubchem.ncbi.nlm.nih.gov/compound/172400033
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| Molecular Formula |
C116H176N32O33.XC2HF3O2
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|---|---|
| Molecular Weight |
2546.86 (free base)
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| Exact Mass |
2546.31111
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| Related CAS # |
Obestatin(human);1081110-72-6
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| SequenceShortening |
FNAPFDVGIKLSGVQYQQHSQAL-NH2
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| Appearance |
Typically exists as solid at room temperature
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| SMILES |
CCC(C)C(C(=NC(CCCCN)C(=NC(CC(C)C)C(=NC(CO)C(=NCC(=NC(C(C)C)C(=NC(CCC(=N)O)C(=NC(CC1=CC=C(C=C1)O)C(=NC(CCC(=N)O)C(=NC(CCC(=N)O)C(=NC(CC2=CN=CN2)C(=NC(CO)C(=NC(CCC(=N)O)C(=NC(C)C(=NC(CC(C)C)C(=N)O)O)O)O)O)O)O)O)O)O)O)O)O)O)O)N=C(CN=C(C(C(C)C)N=C(C(CC(=O)O)N=C(C(CC3=CC=CC=C3)N=C(C4CCCN4C(=O)C(C)N=C(C(CC(=N)O)N=C(C(CC5=CC=CC=C5)N)O)O)O)O)O)O)O
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| InChi Key |
IXQOGPZNKNSCJR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C116H176N32O33/c1-13-61(10)95(146-91(158)53-127-113(178)93(59(6)7)147-110(175)81(50-92(159)160)141-108(173)78(46-65-25-18-15-19-26-65)142-112(177)84-28-22-42-148(84)116(181)63(12)130-105(170)80(49-89(123)156)137-98(163)69(118)45-64-23-16-14-17-24-64)115(180)134-70(27-20-21-41-117)101(166)138-76(44-58(4)5)106(171)143-82(54-149)99(164)126-52-90(157)145-94(60(8)9)114(179)135-74(36-40-88(122)155)104(169)139-77(47-66-29-31-68(151)32-30-66)107(172)132-72(34-38-86(120)153)102(167)131-73(35-39-87(121)154)103(168)140-79(48-67-51-125-56-128-67)109(174)144-83(55-150)111(176)133-71(33-37-85(119)152)100(165)129-62(11)97(162)136-75(96(124)161)43-57(2)3/h14-19,23-26,29-32,51,56-63,69-84,93-95,149-151H,13,20-22,27-28,33-50,52-55,117-118H2,1-12H3,(H2,119,152)(H2,120,153)(H2,121,154)(H2,122,155)(H2,123,156)(H2,124,161)(H,125,128)(H,126,164)(H,127,178)(H,129,165)(H,130,170)(H,131,167)(H,132,172)(H,133,176)(H,134,180)(H,135,179)(H,136,162)(H,137,163)(H,138,166)(H,139,169)(H,140,168)(H,141,173)(H,142,177)(H,143,171)(H,144,174)(H,145,157)(H,146,158)(H,147,175)(H,159,160)
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| Chemical Name |
4-[1-[2-[1-[6-amino-1-[1-[1-[2-[1-[1-[1-[1-[1-[1-[1-[1,5-dihydroxy-1-[1-hydroxy-1-(1-hydroxy-1-imino-4-methylpentan-2-yl)iminopropan-2-yl]imino-5-iminopentan-2-yl]imino-1,3-dihydroxypropan-2-yl]imino-1-hydroxy-3-(1H-imidazol-5-yl)propan-2-yl]imino-1,5-dihydroxy-5-iminopentan-2-yl]imino-1,5-dihydroxy-5-iminopentan-2-yl]imino-1-hydroxy-3-(4-hydroxyphenyl)propan-2-yl]imino-1,5-dihydroxy-5-iminopentan-2-yl]imino-1-hydroxy-3-methylbutan-2-yl]imino-2-hydroxyethyl]imino-1,3-dihydroxypropan-2-yl]imino-1-hydroxy-4-methylpentan-2-yl]imino-1-hydroxyhexan-2-yl]imino-1-hydroxy-3-methylpentan-2-yl]imino-2-hydroxyethyl]imino-1-hydroxy-3-methylbutan-2-yl]imino-3-[[2-[[[1-[2-[[2-[(2-amino-1-hydroxy-3-phenylpropylidene)amino]-1,4-dihydroxy-4-iminobutylidene]amino]propanoyl]pyrrolidin-2-yl]-hydroxymethylidene]amino]-1-hydroxy-3-phenylpropylidene]amino]-4-hydroxybutanoic acid trifluoroacetate salt
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| Synonyms |
Obestatin TFA; Obestatin human(trifluoroacetate salt);
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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 |
| 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.) |
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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