| Size | Price | |
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| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
RKER-216 (0.02–1 μg/mL, 6 hours) has a dissociation constant (KD) of 58.7 pM with ALK2, but it does not bind to ALK3 even at concentrations 10 times higher than those required to bind ALK2 [1]. In ACVR1 knockout in HepG2 and Huh7 cells, there is a potential interaction between RKER-216 and ALK2, with peptide coverage up to 92.2% [1]. RKER-216 (0.02–30 μg/mL, 6 hours) can inhibit alk2-mediated hepcidin transcription in Hep3B cells (0.02–1 μg/mL), HepG2 (ACVR1 knockout) cells (1–30 μg/mL), and Huh7 (ACVR1 knockout) cells (1–30 μg/mL) [1].
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| ln Vivo |
RKER-216 (3 mg/kg, once subcutaneously) inhibits ALK2 without affecting IL-6-mediated hepcidin induction, but reduces total hepcidin secretion in B6N mice by inhibiting the SMAD1/5/9 signaling pathway [1]. RKER-216 (compound m216) (1-3 mg/kg, once subcutaneously, for 6, 24 or 96 hours) inhibits the SMAD signaling pathway, reduces serum hepcidin levels, thereby promoting iron absorption and increasing transferrin saturation (TSAT) in TMPRSS6 KO mice [2]. RKER-216 (1 mg/kg, subcutaneously, twice daily for 9 days) regulates iron metabolism in TMPRSS6 KO mice through a unique mechanism different from intravenous iron [2]. The dose of RKER-216 (1-3 mg/kg, subcutaneously, twice daily for 3 weeks) was proportional to the improvement in microcytic anemia in TMPRSS6 KO mice [2].
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| Cell Assay |
Real-time quantitative PCR[1]
Cell Types: Hep3B, HepG2 (ACVR1 gene knockout) and Huh7 (ACVR1 gene knockout) cell lines Test concentrations: 0.02, 0.2 and 1 μg/mL and 0, 1, 10 and 30 μg/mL Incubation Duration: 6 hours Experimental Results: In Hep3B cells, HAMP mRNA expression decreased in a dose-dependent manner (0.02, 0.2 and 1 μg/mL). At concentrations of 0-1 μg/mL, BMP6-stimulated Hep3B cells showed the strongest inhibitory effect on hepcidin expression, followed by BMP2/6 and BMP2. In HepG2 (ACVR1 knockout (KO)) and Huh7 (ACVR1 knockout (KO)) cell lines, HAMP mRNA levels were not reduced at concentrations of 1–30 μg/mL. |
| Animal Protocol |
Animal/Disease Models:B6N male mice (7 weeks old) [1]
Doses: 3 mg/kg Route of Administration: Subcutaneous injection followed by intraperitoneal injection of LPS (1 mg/kg) Experimental Results: Induced hepatic IL-6 mRNA expression and reduced serum IL-6 levels. Significantly altered Hamp mRNA expression (11.7-fold) and serum hepcidin expression (3.2-fold). Inhibited SMAD1/5/9 phosphorylation, unaffected by inflammatory status. Failed to inhibit LPS-mediated STAT3 phosphorylation; immunoblotting analysis showed the same LPS-induced effect in the isotype control group. Animal/Disease Models:TMPRSS6 KO mice (8-11 weeks old) [2] Doses: 1 or 3 mg/kg Route of Administration: Subcutaneous injection, single dose, administered over 6, 24, or 96 hours Experimental Experimental Results: Six hours after administration of 1 or 3 mg/kg, hepatic smAD1/5/9 phosphorylation, hepcidin (Hamp) mRNA, and serum hepcidin levels decreased. Twenty-four hours after administration of 1 or 3 mg/kg, serum hepcidin decreased by 88%, and TSAT increased 4-fold. 3 mg/kg remained effective 96 hours after administration. |
| References |
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| Molecular Formula |
PLEASEREFERTOTHELOT-SPECIFICCOAFORSPECIFICBUFFERINFORMA
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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.) |
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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