| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
KBP-089 (3 h) can effectively activate human CTR and AMY3-R in heterologous cell lines with pEC50 values ranging from 8.7 to 9.9 and can induce sustained receptor activation for up to 72 hours [1].
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|---|---|
| ln Vivo |
KBP-089 (5 μg/kg; subcutaneous injection; once daily/every other day; for 15 days) produced a similar weight loss effect in rats fed a high-fat diet [1]. KBP-089 (0.625–40 μg/kg; subcutaneous injection; for 6 weeks) reduced body weight and improved glucose tolerance in rats fed a high-fat diet after 4-fold dose escalation [1]. KBP-089 (0.625–40 μg/kg; subcutaneous injection; single dose) dose-dependently suppressed energy intake in overnight fasted high-fat diet rats over 48 hours [1]. KBP-089 (5–20 μg/kg; subcutaneous injection; for 8 weeks) reduced blood glucose levels, improved glucose tolerance and enhanced insulin action in diabetic obese rats [2]. KBP-089 (2.5 µg/kg; subcutaneous injection; for 7 days) reduced total calorie intake in rats on a normal diet and shifted their food preference from chocolate to standard feed [2].
|
| Animal Protocol |
Animal/Disease Models:Sprague Dawley mice (male, 18 weeks old, high-fat diet-induced obesity model) [1]
Doses: 0.625, 2.5, 10, 40 μg/kg Route of Administration: Subcutaneous injection; dose increased 4-fold, followed by maintenance of the final dose for 6 weeks Experimental Results: Transient reduction in food intake was induced at each dose escalation stage (the reduction decreased over time). At doses of 2.5, 10, or 40 μg/kg, approximately 15% body weight loss was achieved (compared to the control group), with corresponding reduction in adipose tissue and improved oral glucose tolerance. Animal/Disease Models:Zucker diabetic obese (ZDF-Leprfa/Crl) rats (male, 6 weeks old) [2] Doses: 5 µg/kg (first 4 weeks) and 20 µg/kg (last 4 weeks) Route of Administration: Subcutaneous injection; once daily; for 8 weeks Experimental Results: Fasting blood glucose decreased within 7 weeks. Glycated hemoglobin (HbA1c) decreased at the end of the study; area under the curve (tAUC) of oral glucose tolerance test decreased. Insulin sensitivity increased. |
| References |
|
| Molecular Formula |
C148H242N46O48S3
|
|---|---|
| Molecular Weight |
3529.98
|
| CAS # |
1776112-67-4
|
| Sequence |
Ac-Cys-Ser-Asn-Leu-Ser-Thr-Cys-Met-Leu-Gly-Arg-Leu-Ser-Gln-Asp-Leu-His-Arg-Leu-Gln-Thr-Tyr-Pro-Lys-Thr-Asp-Val-Gly-Ala-Asn-Ala-Pro-NH2 (Disulfide bridge: Cys1-Cys7)Ac-CSNLSTCMLGRLSQDLHRLQTYPKTDVGANAP-NH2 (Disulfide bridge: Cys1-Cys7)
|
| SequenceShortening |
Ac-CSNLSTCMLGRLSQDLHRLQTYPKTDVGANAP-NH2 (Disulfide bridge: Cys1-Cys7)
|
| Appearance |
Typically exists as solids at room temperature
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| 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 | 0.2833 mL | 1.4164 mL | 2.8329 mL | |
| 5 mM | 0.0567 mL | 0.2833 mL | 0.5666 mL | |
| 10 mM | 0.0283 mL | 0.1416 mL | 0.2833 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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