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| 5mg |
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| Targets |
Seliforant targets the histamine H4 receptor. It is a selective antagonist of this receptor. The H4 receptor is a G-protein coupled receptor that is involved in immune responses, inflammation, and, as recently discovered, vestibular function. By blocking the H4 receptor, Seliforant modulates these processes.
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| ln Vitro |
Seliforant is a potent antagonist of the histamine H4 receptor. Its in vitro activity is characterized by its ability to bind to the H4 receptor and block its activation. Specific IC50 or Ki values are not provided in the search results. However, it is described as a novel and potent antagonist.
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| ln Vivo |
Seliforant has demonstrated in vivo activity in a rat model of vertigo. Selective inhibition of the H4 receptor improves vertigo symptoms in rats with unilateral vestibular lesions. This confirms its efficacy in a relevant animal model and suggests its potential for treating vestibular disorders.
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| Enzyme Assay |
The in vitro activity of Seliforant is assessed using radioligand binding assays. The compound is tested for its ability to displace a labeled ligand from the histamine H4 receptor. Its selectivity is confirmed by testing against other histamine receptor subtypes.
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| Cell Assay |
The antagonist activity of Seliforant is confirmed in functional cell-based assays. Cells expressing the H4 receptor are stimulated with a histamine H4 agonist in the presence of various concentrations of Seliforant. The compound's ability to block the agonist-induced response, such as calcium mobilization or other signaling events, is measured.
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| Animal Protocol |
In vivo studies have been conducted in a rat model of unilateral vestibular lesions. In these experiments, rats with induced vestibular lesions are treated with Seliforant, and their vertigo symptoms are assessed. The compound's ability to improve these symptoms confirms its efficacy in modulating vestibular function.
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| ADME/Pharmacokinetics |
Seliforant has a molecular weight of 235.33 and a molecular formula of C12H21N5. Its IUPAC name is 2-isobutyl-6-(3-(methylamino)azetidin-1-yl)pyrimidin-4-amine. It is a selective and orally active histamine H4 receptor antagonist. It is also known as SENS-111. It is soluble in DMSO.
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| Toxicity/Toxicokinetics |
Seliforant is a research compound, and its toxicity profile is not detailed in the provided sources. As a selective H4 receptor antagonist, it is expected to have a more targeted mechanism of action and potentially fewer off-target effects. However, comprehensive toxicology studies would be required for its development.
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| References |
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| Additional Infomation |
Seliforant is being investigated in the clinical trial NCT01260753 (UR-63325 activity validation study for the treatment of nasal provocation-induced allergic rhinitis).
Seliforant (CAS#: 1164115-89-2) is a novel and potent histamine H4 receptor antagonist, also known as SENS-111. It is a selective and orally active antagonist. Histamine H4 receptors are expressed in the peripheral vestibular system, and their selective inhibition improves vertigo symptoms in rats with unilateral vestibular lesions. Seliforant is a research tool for studying H4 receptor function and potential therapeutic applications in vestibular disorders. |
| Molecular Formula |
C12H21N5
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|---|---|
| Molecular Weight |
235.34
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| Exact Mass |
235.179
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| Elemental Analysis |
C, 61.25; H, 8.99; N, 29.76
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| CAS # |
1164115-89-2
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| PubChem CID |
44126305
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| Appearance |
Light brown to brown ointment
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
412.9±45.0 °C at 760 mmHg
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| Flash Point |
203.5±28.7 °C
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| Vapour Pressure |
0.0±1.0 mmHg at 25°C
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| Index of Refraction |
1.576
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| LogP |
-0.18
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
17
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| Complexity |
239
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| Defined Atom Stereocenter Count |
0
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| SMILES |
N1(C2C=C(N)N=C(CC(C)C)N=2)CC(C1)NC
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| InChi Key |
QRBVUFXEMHNIDB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C12H21N5/c1-8(2)4-11-15-10(13)5-12(16-11)17-6-9(7-17)14-3/h5,8-9,14H,4,6-7H2,1-3H3,(H2,13,15,16)
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| Chemical Name |
6-[3-(methylamino)azetidin-1-yl]-2-(2-methylpropyl)pyrimidin-4-amine
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| Synonyms |
SENS-111; SENS 111; Seliforant; 1164115-89-2; B61N8R7TDH; 2-Isobutyl-6-(3-(methylamin)azetidin-1-yl)pyrimidin-4-amine; 6-(3-(Methylamino)-1-azetidinyl)-2-(2-methylpropyl)-4-pyrimidinamine; SENS111
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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) |
DMSO : ~100 mg/mL (~424.94 mM)
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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 | 4.2492 mL | 21.2459 mL | 42.4917 mL | |
| 5 mM | 0.8498 mL | 4.2492 mL | 8.4983 mL | |
| 10 mM | 0.4249 mL | 2.1246 mL | 4.2492 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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