| Size | Price | Stock | Qty |
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| 100mg |
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| 500mg | |||
| 1g | |||
| Other Sizes |
| Targets |
Histamine N-methyltransferase (HMT). SKF 91488 is a noncompetitive inhibitor of this enzyme, with a Ki value of 0.9 microM. By inhibiting HMT, it prevents the methylation of histamine, leading to increased levels of endogenous histamine in tissues and prolonging its biological effects, which include neurotransmission, gastric acid secretion, and immune modulation.
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| ln Vitro |
SKF 91488 inhibits the methylation of labeled histamine in mice. In cell-free assays, it demonstrates potent noncompetitive inhibition of human HMT with a reported Ki of 0.9 microM. It also inhibits rat kidney HMT in a time- and concentration-dependent manner. It is one of the most widely used pharmacological tools for HMT inhibition.
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| ln Vivo |
In vivo, SKF 91488 dihydrochloride inhibits the methylation of labeled histamine in mice. By blocking histamine degradation, it elevates histamine levels in various tissues. This has been used in pharmacological studies to elucidate the role of HMT in regulating histamine-mediated physiological responses, such as gastric acid secretion and central nervous system activity.
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| Enzyme Assay |
SKF 91488 is a noncompetitive inhibitor. For in vitro binding and inhibition studies, histamine N-methyltransferase (HMT) enzyme (e.g., from rat kidney or human recombinant) is incubated with various concentrations of SKF 91488 (0.1-100 uM) in a reaction buffer (sodium phosphate buffer, pH 7.4). The reaction is started by adding the substrate histamine (1-100 uM) and the methyl donor 3H-S-adenosyl methionine (SAM). After 30-60 minutes at 37degC, the reaction is stopped with perchloric acid. The radiolabeled product (3H-methylhistamine) is extracted into an organic solvent and counted by scintillation. Ki and IC50 are determined using Lineweaver-Burk and Dixon plot analyses.
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| Cell Assay |
For cell culture studies, cell lines that express HMT (e.g., HeLa cells, rat basophilic leukemia RBL-2H3 cells) are seeded in 6- or 96-well plates. Cells are treated with varying concentrations of SKF 91488 (1-100 uM) for 30-60 minutes. To assess HMT inhibition, cells are incubated with 3H-histamine for 1 hour. The amount of 3H-methylhistamine produced is measured in the cell supernatant or lysates after separation by organic extraction. Alternatively, histamine levels in the culture medium can be measured directly by ELISA. For functional assays, histamine release is induced by ionophore A23187 or IgE crosslinking.
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| Animal Protocol |
A typical protocol for in vivo studies involves administering SKF 91488 dihydrochloride to male Swiss-Webster mice (25-30 g) via intraperitoneal (i.p.) injection at doses ranging from 1-50 mg/kg, often 30-60 minutes prior to histamine challenge or tracer administration. Blood and tissues (brain, stomach) are collected, and histamine levels or the methylation of 3H-histamine are measured. For gastric acid secretion studies, the compound can be administered i.p., and stomach contents are collected to measure pH and acid output.
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| ADME/Pharmacokinetics |
SKF 91488 is a small molecule (MW 248.22 g/mol) that is likely well-distributed throughout the body, including the central nervous system, due to its moderate lipophilicity. Specific pharmacokinetic parameters (e.g., t½, Cmax, AUC) have not been published for this compound. Its pharmacodynamic effects correlate with the inhibition of HMT activity.
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| Toxicity/Toxicokinetics |
No formal toxicological data is available for SKF 91488. As an HMT inhibitor, it is generally well-tolerated in acute animal studies at pharmacologically active doses (1-50 mg/kg). Potential toxicity would be related to an exaggerated pharmacological effect, such as excessive gastric acid secretion, central nervous system stimulation (due to elevated neuronal histamine), or hypotension from peripheral histamine accumulation. For research use only.
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| References | |
| Additional Infomation |
SKF 91488 is also known by the synonym Homodimaprit. It has been a critical research tool for over four decades, allowing scientists to study the physiological and pathological roles of histamine in the absence of H1/H2 receptor antagonists. By inhibiting degradation, it specifically elevates endogenous histamine levels, distinguishing it from receptor agonists. Its chemical name is 4-(dimethylamino)butyl carbamimidothioate dihydrochloride; molecular formula: C7H19Cl2N3S.
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| Molecular Formula |
C7H19CL2N3S
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|---|---|
| Molecular Weight |
248.22
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| Exact Mass |
211.091
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| Elemental Analysis |
C, 33.87; H, 7.72; Cl, 28.56; N, 16.93; S, 12.92
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| CAS # |
68941-21-9
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| PubChem CID |
11957708
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| Appearance |
White to off-white solid powder
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| LogP |
2.556
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
13
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| Complexity |
114
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| Defined Atom Stereocenter Count |
0
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| SMILES |
Cl.Cl.CN(CCCCSC(=N)N)C
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| InChi Key |
NPLHSMBWWIIWAQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C7H17N3S.2ClH/c1-10(2)5-3-4-6-11-7(8)9;;/h3-6H2,1-2H3,(H3,8,9);2*1H
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| Chemical Name |
4-(dimethylamino)butyl carbamimidothioate dihydrochloride
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| Synonyms |
SKF 91488 dihydrochloride; SKF 91488 HCl; SKF91488 HCl; SKF 91488 dihydrochloride
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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 | 4.0287 mL | 20.1434 mL | 40.2868 mL | |
| 5 mM | 0.8057 mL | 4.0287 mL | 8.0574 mL | |
| 10 mM | 0.4029 mL | 2.0143 mL | 4.0287 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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