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| 100mg |
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| 250mg |
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Buformin (NSC-528218; 1-butylbiguanide) is an orally bioavailable AMPK activator approved for use as an antidiabetic drug. It is structurally related to metformin and phenformin and is a member of the biguanide class. Buformin works in vivo by reducing blood glucose synthesis and hepatic gluconeogenesis. Silubin, a brand name for buformin, was sold by the German pharmaceutical company Grünenthal. Buformin increases insulin sensitivity and glucose uptake into cells, delays gastrointestinal absorption of glucose, and prevents the liver from synthesizing glucose. The biguanides, including buformin, are antihyperglycemic rather than hypoglycemic medications. They lessen basal and postprandial hyperglycemia in diabetics rather than causing hypoglycemia. Biguanides may counteract glucagon's effects, lowering fasting glucose levels.
| ln Vitro |
Buformin (0–10 mM; 5 days) inhibits the growth of SKBR3 and BT474 cells in a concentration-dependent manner; the IC50 values for erbB-2–overexpressing SKBR3 and BT474 cells are 246.7 M and 98.6 M, respectively[1]. Buformin (0-3 mM; 48 hours) increases the percentage of cells in G0/G1 phase and reduced the percentage of cells in S phase, especially in the SKBR3 cells[1]. Buformin (0–3 mM; 24 hours) inhibits Akt activation/phosphorylation in both SKBR3 and BT474 cells and suppresses RTK activation, including erbB-2 and IGF1R signaling downstream[1].
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| ln Vivo |
Buformin (oral administation; 7.6 mmol/kg of chow; 7 days) has significantly decreased tumor weights and volumes, and MMTV-erbB-2 transgenic mice show decreased mammary morphogenesis and proliferation[1].
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| References |
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| Molecular Formula |
C6H15N5
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|---|---|
| Molecular Weight |
157.2168
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| Exact Mass |
157.1327
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| Elemental Analysis |
C, 45.84; H, 9.62; N, 44.55
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| CAS # |
692-13-7
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| Related CAS # |
Buformin hydrochloride;1190-53-0;Buformin-d9 hydrochloride
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| Appearance |
Solid powder
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| SMILES |
N=C(NC(N)=N)NCCCC
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| InChi Key |
XSEUMFJMFFMCIU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C6H15N5/c1-2-3-4-10-6(9)11-5(7)8/h2-4H2,1H3,(H6,7,8,9,10,11)
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| Chemical Name |
1-Butylbiguanide
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| Synonyms |
Buformin; W-37; W37; W 37; H 224
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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 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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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 6.3605 mL | 31.8026 mL | 63.6051 mL | |
| 5 mM | 1.2721 mL | 6.3605 mL | 12.7210 mL | |
| 10 mM | 0.6361 mL | 3.1803 mL | 6.3605 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.
| NCT Number | Status | Interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT01584232 | Completed | Drug: LY2189265 Drug: Insulin glargine |
Type 2 Diabetes Mellitus | Eli Lilly and Company | April 2012 | Phase 3 |
| NCT02476760 | Completed | Drug: Insulins Drug: DPP-4 inhibitors |
Diabetes Mellitus, Type 2 | Canadian Network for Observational Drug Effect Studies, CNODES |
March 2014 |
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