| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
KBP-066A (0-25 μM) binds to AMY3R in a concentration-dependent manner [1]. KBP-066A activates CTR (U20S CALCR) and AMY3R (CHO K1 CALCR RAMP3) cells and has no off-target activity against the tested calcitonin-like receptor [1].
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| ln Vivo |
KBP-066A (1-4 nmol/kg; subcutaneous injection; every three days; for 4 weeks) significantly reduced the body weight of obese rats in a dose-dependent manner and improved their glycemic control [1]. KBP-066A (0.75-3 nmol/kg; subcutaneous injection; every three days; for 8 weeks) improved the glycemic status of diabetic ZDF rats [1]. KBP-066A (0.5-36 nmol/kg; subcutaneous injection; single dose) had a dose-dependent acute effect on obese rats, reducing their food intake and body weight, with the high-dose group showing a longer duration of effect [1].
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| Animal Protocol |
Animal/Disease Models:Sprague Dawley (male, 5-6 weeks old at arrival, baseline weight of 528.2 ± 27.9 g at the start of the study, who was made obese by a 60 kcal% high-fat diet for 20 weeks) [1]
Doses: 1, 2, 4 nmol/kg Route of Administration: Subcutaneous injection; every three days; for 4 weeks Experimental Results: Compared with the vector group (2773 ± 4 g/day), the body weight tAUC decreased to 2584 ± 7, 2452 ± 6, and 2458 ± 8 g/day. Compared with the control group (811 ± 11 g/day), the cumulative food intake tAUC of each group decreased to 617 ± 10, 518 ± 6, and 532 ± 10 g/day, respectively. Perirenal adipose tissue was reduced in the 2 nmol/kg and 4 nmol/kg groups. Oral glucose tolerance improved (iAUC was not significantly different compared with the control group). Plasma insulin iAUC and HOMA-IR were significantly reduced. Animal/Disease Models:Zucker diabetic fat rats (ZDF) (male, 5-6 weeks old at arrival, baseline weight 334.1 ± 15.5 g, baseline fasting blood glucose 14 ± 5.1 mM, baseline plasma insulin 8.0 ± 3.9 ng/mL) [1] Doses: 0.75, 1.5, 3 nmol/kg Route of Administration: Subcutaneous injection; once every three days; 8 weeks Experimental Results: Fasting blood glucose tAUC decreased to 6180±67, 6405±89, 6409±122, while the control group was 6475±103. Cumulative food intake (tAUC) decreased to 3815±135, 3134±111, and 2898±61 gdays⁻¹, respectively, compared to 4453±123 gdays⁻¹ in the control group. HbA1c decreased, and the oral glucose tolerance test (iAUC) significantly improved at a dose of 3 nmol/kg. No significant weight loss was observed. |
| References |
| Molecular Formula |
C182H303N47O60S2
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|---|---|
| Molecular Weight |
4173.76
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| Sequence |
Ac-Cys-Ser-Asn-Leu-Ser-Thr-Cys-{Aib}-Leu-Gly-{Lys(2OEG-γGlu-C18 diacid)}-Leu-Ser-Gln-Asp-Leu-His-Arg-Leu-Gln-Thr-Tyr-Pro-Lys-Thr-Asp-Val-Gly-Ala-Asn-Ala-Pro-NH2Ac-CSNLSTC-{Aib}-LG-{K(2OEG-γGlu-C18 diacid)}-LSQDLHRLQTYPKTDVGANAP-NH2
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| SequenceShortening |
Ac-CSNLSTC-{Aib}-LG-{K(2OEG-γGlu-C18 diacid)}-LSQDLHRLQTYPKTDVGANAP-NH2
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| Appearance |
Typically exists as solids at room temperature
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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 | 0.2396 mL | 1.1980 mL | 2.3959 mL | |
| 5 mM | 0.0479 mL | 0.2396 mL | 0.4792 mL | |
| 10 mM | 0.0240 mL | 0.1198 mL | 0.2396 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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