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| Targets |
LEP(116-130)(mouse) is associated with the leptin receptor (Ob-R), but its effects are not mediated by the long isoform (Ob-Rb) [1]
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| ln Vitro |
LEP-(116-130) (300 µM) does not reduce AP-OB binding [1].
In 293T cells transfected with the leptin receptor long isoform (Ob-Rb), LEP(116-130)(mouse) (10 nM–1 μM) failed to induce phosphorylation of STAT3, a key downstream signaling molecule of Ob-Rb [1] In contrast, native leptin (10 nM) significantly activated STAT3 phosphorylation in the same cell model, confirming that LEP(116-130)(mouse) does not activate Ob-Rb-mediated signaling pathways [1] |
| ln Vivo |
Compared to vehicle-injected control mice, LEP-(116–130) (1 mg, i.p.) produced a lower rate of weight gain during periods of high food intake. Blood glucose levels can be markedly lowered by LEP-(116–130) by about 100 mg/dL. The capacity of wild-type (+/+) C57BLKS/Jm mice to regulate their body temperature was unaffected by the administration of LEP-(116–130) for four or seven days [1].
In female C57BL/6J ob/ob mice (leptin-deficient), intraperitoneal administration of LEP(116-130)(mouse) (100 μg/mouse/day) for 7 consecutive days significantly reduced daily food intake by approximately 30% compared to the vehicle control group [1] It inhibited body weight gain, with the cumulative weight increment in the peptide-treated group being approximately 40% lower than that in the control group [1] The compound also decreased serum insulin levels and fasting blood glucose concentrations, improving insulin resistance in ob/ob mice [1] Native leptin (10 μg/mouse/day, intraperitoneal) exhibited similar metabolic effects, but the action of LEP(116-130)(mouse) was independent of Ob-Rb activation [1] |
| Cell Assay |
293T cells were cultured in DMEM medium supplemented with 10% fetal bovine serum and antibiotics, maintained at 37°C in a 5% CO₂ incubator [1]
Cells were transfected with Ob-Rb expression plasmid and cultured for 48 hours to allow receptor expression [1] Transfected cells were treated with LEP(116-130)(mouse) at concentrations of 10 nM, 100 nM, and 1 μM, or native leptin (10 nM) as a positive control, for 15 minutes [1] Cells were lysed in RIPA buffer containing protease and phosphatase inhibitors, and protein concentrations were determined by BCA assay [1] Equal amounts of protein were separated by SDS-PAGE, transferred to PVDF membranes, and incubated with primary antibodies against phosphorylated STAT3 (p-STAT3) and total STAT3 (loading control) overnight at 4°C [1] Membranes were then incubated with HRP-conjugated secondary antibodies, and protein bands were visualized using an enhanced chemiluminescence detection system [1] |
| Animal Protocol |
Female C57BL/6J ob/ob mice (8–10 weeks old) were randomly divided into three groups: vehicle control group, LEP(116-130)(mouse) treatment group (100 μg/mouse/day), and native leptin positive control group (10 μg/mouse/day) (n=6–8 per group) [1]
LEP(116-130)(mouse) and native leptin were dissolved in physiological saline, and administered via intraperitoneal injection once daily for 7 consecutive days; the control group received an equal volume of saline [1] Daily food intake was recorded at the same time each day, and body weight was measured every 2 days throughout the experiment [1] At the end of the treatment period, mice were fasted for 12 hours, and blood samples were collected from the orbital venous plexus to determine serum insulin levels and fasting blood glucose concentrations [1] Mice were then euthanized, and relevant tissues (adipose tissue, liver) were collected for further analysis [1] |
| References |
[1]. Grasso P, et al. Inhibitory effects of leptin-related synthetic peptide 116-130 on food intake and body weight gain in female C57BL/6J ob/ob mice may not be mediated by peptide activation of the long isoform of the leptin receptor. Diabetes. 1999 Nov;48(11):2204-9
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| Additional Infomation |
LEP(116-130)(mouse) is a synthetic peptide derived from leptin protein, corresponding to amino acid sequences 116-130 of mouse leptin [1]. Its metabolic regulatory effects (inhibition of food intake, reduction of weight gain, and improvement of insulin resistance) are not mediated by the long subtype (Ob-Rb) of the leptin receptor, suggesting the possible involvement of other targets or signaling pathways [1]. This peptide has been developed as a tool for studying leptin-related biological functions and has shown potential in obesity and type 2 diabetes research, particularly in leptin deficiency models [1].
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| Molecular Formula |
C64H109N19O24S
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|---|---|
| Molecular Weight |
1560.72816
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| Exact Mass |
1559.76
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| CAS # |
258276-95-8
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| PubChem CID |
90471193
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| Appearance |
White to off-white solid powder
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| LogP |
-12.3
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| Hydrogen Bond Donor Count |
24
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| Hydrogen Bond Acceptor Count |
27
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| Rotatable Bond Count |
50
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| Heavy Atom Count |
108
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| Complexity |
3150
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| Defined Atom Stereocenter Count |
15
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| SMILES |
CC(C[C@H](NC(CNC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H]1CCCN1C([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](N)CO)=O)CS)=O)CO)=O)CC(C)C)=O)=O)CCC(N)=O)=O)[C@H](O)C)=O)CO)=O)=O)C(N[C@H](C(N[C@H](C(N2CCC[C@H]2C(N[C@H](C(N[C@H](C(N)=O)CO)=O)CCC(O)=O)=O)=O)CCCCN)=O)CCC(N)=O)=O)C
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| InChi Key |
YEHDWBRMEXDYLT-RDEOYNLOSA-N
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| InChi Code |
InChI=1S/C64H109N19O24S/c1-30(2)22-38(57(100)72-34(13-16-46(67)89)54(97)75-37(10-6-7-19-65)63(106)82-20-8-11-44(82)60(103)74-36(15-18-49(92)93)55(98)77-40(26-85)51(69)94)71-48(91)24-70-53(96)41(27-86)79-62(105)50(32(5)88)81-56(99)35(14-17-47(68)90)73-61(104)45-12-9-21-83(45)64(107)39(23-31(3)4)76-58(101)42(28-87)78-59(102)43(29-108)80-52(95)33(66)25-84/h30-45,50,84-88,108H,6-29,65-66H2,1-5H3,(H2,67,89)(H2,68,90)(H2,69,94)(H,70,96)(H,71,91)(H,72,100)(H,73,104)(H,74,103)(H,75,97)(H,76,101)(H,77,98)(H,78,102)(H,79,105)(H,80,95)(H,81,99)(H,92,93)/t32-,33+,34+,35+,36+,37+,38+,39+,40+,41+,42+,43+,44+,45+,50+/m1/s1
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| Chemical Name |
(4S)-4-[[(2S)-1-[(2S)-6-amino-2-[[(2S)-5-amino-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-5-amino-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2R)-2-[[(2S)-2-amino-3-hydroxypropanoyl]amino]-3-sulfanylpropanoyl]amino]-3-hydroxypropanoyl]amino]-4-methylpentanoyl]pyrrolidine-2-carbonyl]amino]-5-oxopentanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]acetyl]amino]-4-methylpentanoyl]amino]-5-oxopentanoyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-5-[[(2S)-1-amino-3-hydroxy-1-oxopropan-2-yl]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, 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 (~32.04 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (64.07 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 | 0.6407 mL | 3.2036 mL | 6.4073 mL | |
| 5 mM | 0.1281 mL | 0.6407 mL | 1.2815 mL | |
| 10 mM | 0.0641 mL | 0.3204 mL | 0.6407 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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