| Size | Price | |
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| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
REGN7999 can block the activity of human and mouse TMPRSS6 in HEK293 cells overexpressing HJV and TMPRSS6, with IC50 values of 0.68 and 16 nM, respectively, and can prevent HJV cleavage [2]. REGN7999 can bind to TMPRSS6 and inhibit cross-species TMPRSS6 activity, reducing the proteolytic activity of human reference and variant TMPRSS6, cynomolgus monkey TMPRSS6, and mouse TMPRSS6 [2].
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| ln Vivo |
REGN7999 (10 mg/kg, subcutaneous injection, once a week for 12 weeks) increased serum hepcidin levels, decreased liver iron content, restored red blood cell (RBC) levels, and improved red blood cell health in the Hbbth3/+ model [1][2]. REGN7999 (5 mg/kg, subcutaneous injection, once a week) increased serum hepcidin and decreased serum iron in the C57BL/6 model [2].
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| Animal Protocol |
Animal/Disease Models: Hbbth3/+ mice model[1][2]
Doses: 10 mg/kg Route of Administration: s.c., once a week, 12 weeks Experimental Results: Reduced liver iron (~50% reduction compared to the isotype-treated group), improved RBC health as determined by reduced annexin V staining and RBC turnover, extend the RBC life span. Elevated serum hepcidin and hepatic HAMP1 expression, did not increase markers of liver damage. Reduced spleen weights to WT levels, displayed normalized reticulocyte numbers, blunted the increase in oxidative stress in blood and spleens, reduced bilirubin levels and lower expression levels of hepatic Hmox1, improved anaerobic capacity, increased bone mineral density. Animal/Disease Models: C57BL/6 mice model[2] Doses: 5 mg/kg Route of Administration: s.c., once Experimental Results: Increased serum hepcidin, and decreased in serum iron, led to a significant drop of transferrin saturation and serum iron in the first 24 hours. |
| References |
| 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.) |
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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