| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
The full-length obestatin peptide was originally proposed to target the G-protein coupled receptor GPR39, though this remains controversial and the molecular mechanism for obestatin's effects in vivo is still uncertain . Through NMR conformational analysis, the C-terminal region of obestatin (which constitutes this fragment) has been shown to contain structural elements similar to other GPCR-binding neuropeptides, supporting its identity as a GPCR ligand .
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|---|---|
| ln Vitro |
Using CD and NMR conformational analysis, Obestatin(11-23) has been shown to assume a regular secondary structure in the C-terminal region of the molecule. This structural feature is similar to other GPCR-binding neuropeptides, supporting the identity of obestatin as a new and functionally autonomous GPCR ligand .
|
| ln Vivo |
In mice, a single intraperitoneal administration of obestatin (11-23) at a dose of 1 μmol/kg significantly reduces food intake compared to saline controls, with a 53% reduction in feeding observed over a 15-minute period. The reduction in food intake is accompanied by secondary decreases in glucose excursions and insulin responses. The peptide has no direct effects on glucose homeostasis, insulin secretion, or insulin sensitivity independent of its anorectic actions .
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| Enzyme Assay |
While specific radioligand binding assays for this fragment are not detailed in the available sources, the NMR structural analysis of Obestatin(11-23) was performed in DPC/SDS micellar solutions to mimic membrane environments, revealing that the C-terminal region contains structural elements similar to other GPCR-binding neuropeptides. This supports its potential role as a GPCR ligand .
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| Animal Protocol |
In the acute feeding study, male mice were administered obestatin (11-23) via intraperitoneal (IP) injection at a dose of 1 μmol/kg. Food intake was measured 4 hours post-injection during an allowed 15-minute feeding period. The obestatin fragment was dissolved in saline for administration .
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| ADME/Pharmacokinetics |
The full-length obestatin peptide is known to have biological instability, with rapid enzymatic cleavage demonstrated in liver homogenates. However, the C-terminal fragment (11-23) may exhibit different stability characteristics. The molecular formula of this fragment is C₆₁H₉₈N₂₂O₁₈, with a molecular weight of 1427.57 g/mol. For reconstitution, stock solutions once prepared should be stored in aliquoted, tightly sealed vials and used within 1 month. Repeated freeze and thaw cycles should be avoided .
|
| References |
| Molecular Formula |
C61H98N22O18
|
|---|---|
| Molecular Weight |
1427.57
|
| Exact Mass |
1426.743
|
| CAS # |
938193-98-7
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| PubChem CID |
169450771
|
| Sequence |
Leu-Ser-Gly-Ala-Gln-Tyr-Gln-Gln-His-Gly-Arg-Ala-Leu-NH2
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| SequenceShortening |
LSGAQYQQHGRAL-NH2
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| Appearance |
Typically exists as solid at room temperature
|
| Hydrogen Bond Donor Count |
22
|
| Hydrogen Bond Acceptor Count |
21
|
| Rotatable Bond Count |
47
|
| Heavy Atom Count |
101
|
| Complexity |
2890
|
| Defined Atom Stereocenter Count |
11
|
| SMILES |
O=C([C@H](CCC(N)=O)NC([C@H](CC1C=CC(=CC=1)O)NC([C@H](CCC(N)=O)NC([C@H](C)NC(CNC([C@H](CO)NC([C@H](CC(C)C)N)=O)=O)=O)=O)=O)=O)N[C@H](C(N[C@H](C(NCC(N[C@H](C(N[C@@H](C)C(N[C@H](C(N)=O)CC(C)C)=O)=O)CCC/N=C(\N)/N)=O)=O)CC1=CN=CN1)=O)CCC(N)=O
|
| InChi Key |
NDWBQTKASKXOCL-MGFBIKGDSA-N
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| InChi Code |
InChI=1S/C61H98N22O18/c1-29(2)20-36(62)53(94)83-44(27-84)55(96)72-25-48(89)74-31(5)51(92)77-38(13-16-45(63)86)58(99)81-42(22-33-9-11-35(85)12-10-33)60(101)79-39(14-17-46(64)87)57(98)78-40(15-18-47(65)88)59(100)82-43(23-34-24-69-28-73-34)54(95)71-26-49(90)76-37(8-7-19-70-61(67)68)56(97)75-32(6)52(93)80-41(50(66)91)21-30(3)4/h9-12,24,28-32,36-44,84-85H,7-8,13-23,25-27,62H2,1-6H3,(H2,63,86)(H2,64,87)(H2,65,88)(H2,66,91)(H,69,73)(H,71,95)(H,72,96)(H,74,89)(H,75,97)(H,76,90)(H,77,92)(H,78,98)(H,79,101)(H,80,93)(H,81,99)(H,82,100)(H,83,94)(H4,67,68,70)/t31-,32-,36-,37-,38-,39-,40-,41-,42-,43-,44-/m0/s1
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| Chemical Name |
(2S)-N-[(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-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-3-(1H-imidazol-5-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]-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-amino-4-methylpentanoyl]amino]-3-hydroxypropanoyl]amino]acetyl]amino]propanoyl]amino]pentanediamide
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| Synonyms |
Obestatin(11-23)mouse, rat; Obestatin(11-23) (mouse, rat)
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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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.7005 mL | 3.5025 mL | 7.0049 mL | |
| 5 mM | 0.1401 mL | 0.7005 mL | 1.4010 mL | |
| 10 mM | 0.0700 mL | 0.3502 mL | 0.7005 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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