| Size | Price | |
|---|---|---|
| 1mg | ||
| 5mg | ||
| Other Sizes |
| Targets |
KD: 0.1 nM[2]
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|---|---|
| ln Vitro |
Crotedumab has a high affinity (KD=0.03 nM-0.39 nM) for binding GCGR from several species, including humans, rats, mice, and monkeys [2]. With IC50 values of 0.65, 3.2, 0.94, and 1.0 nM, respectively, crotedumab inhibits glucagon-induced signaling through GCGR in HEK293 cells transfected with human, monkey, mouse, and rat GCGR [2].
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| ln Vivo |
In rodents with diet-induced obesity, crotedumab (3-30 mg/kg; subcutaneous injection once weekly for 4 weeks) lowers blood glucose and body weight and causes reversible hyperglucagonemia and alpha-cell hyperplasia[2]. For eighteen days, diabetic ob/ob mice receiving a single subcutaneous injection of crotedumab (10 mg/kg) have significantly lower blood glucose levels[2]. In both conscious and unconscious diabetic cynomolgus monkeys, REGN1193 (20 mg/kg; single intravenous injection) dramatically lowers blood glucose levels assessed an hour after feeding and during nocturnal fasting[2].
|
| Animal Protocol |
Animal/Disease Models: Diet-induced obese (DIO) male C57BL/6NTac mice were maintained on high-fat diet[2]
Doses: 3, 10, 30 mg/kg Route of Administration: Sc injection once weekly for 4 weeks Experimental Results: Markedly decreased blood glucose Throughout the dosing period. Reversibly diminished body weight during the dosing period. Dose- and time-dependently increased glucagon and GLP-1. Reversibly increased α-cell area. |
| References |
[1]. Kostic A, et, al. A first-in-human pharmacodynamic and pharmacokinetic study of a fully human anti-glucagon receptor monoclonal antibody in normal healthy volunteers. Diabetes Obes Metab. 2018 Feb;20(2):283-291.
[2]. Okamot H, et, al. Glucagon Receptor Blockade With a Human Antibody Normalizes Blood Glucose in Diabetic Mice and Monkeys. Endocrinology. 2015 Aug;156(8):2781-94. |
| CAS # |
1452387-69-7
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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.) |
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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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