Seliforant
Based on 1 Customer Validation
Seliforant (SENS-111) is a selective, orally active histamine H4 receptor antagonist. Seliforant inhibits the sustained activity of vestibular neurons and modulates vestibular-related responses. Seliforant reduces spontaneous nystagmus in rats with excitotoxic acute unilateral vestibular loss. Seliforant shows no sedative effect. Seliforant can be used in research related to acute unilateral vestibular loss, vestibular dysfunction, and acute unilateral vestibular lesions.
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- Purity: 95.0%
- CAS No.: 1164115-89-2
- 화학식: C12H21N5
- 분자량:235.33
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보관:Pure form -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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All Histamine Receptor Isoforms
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Biological Activity
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H4 receptor |
Seliforant (at levels corresponding to plasma concentrations of 60-150 ng mL-1) antagonizes histamine H4 receptor activity in inner ear tissues[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Seliforant (SENS-111) (10 mg·kg−1; i.v.; single dose) produces a statistically significant 21% reduction in normalized spontaneous nystagmus frequency in rats with acute unilateral vestibular loss, maintains a significant 15% reduction when co-administered with methylprednisolone, but loses efficacy when co-administered with meclizine[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Long-Evans (12-week-old female, ~175-200 g, acute unilateral vestibular loss induced via two transtympanic injections of kainic acid)[1]
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Dosage:10 mg·kg-1; 20 mg·kg-1
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Administration:i.v.; single dose
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Result:Reduced normalized spontaneous nystagmus frequency by a statistically significant 22% at the peak of vertigo symptoms (1 hour after baseline recording and treatment) at 10 mg·kg-1 dose, almost abolishing symptom worsening seen in vehicle controls.
Showed a non-significant 12% reduction in normalized spontaneous nystagmus frequency compared to vehicle controls at 20 mg·kg-1 dose.
Reached plasma concentrations of 112 ng·mL-1 3 hours post-administration at 10 mg·kg-1 dose.
Reached plasma concentrations of 319 ng·mL-1 3 hours post-administration at 20 mg·kg-1 dose.
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Animal Model:Long-Evans (12-week-old female, ~175-200 g, acute unilateral vestibular loss induced via a single transtympanic injection of kainic acid)[1]
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Dosage:10 mg·kg-1; 10 mg·kg-1 + 5.2 mg·kg-1 meclizine; 10 mg·kg-1 + 6.2 mg·kg-1 methylprednisolone
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Administration:i.v.; single dose; i.p. (meclizine, methylprednisolone)
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Result:Reduced normalized spontaneous nystagmus frequency by a statistically significant 21% at the peak of vertigo symptoms (1 hour after treatment) when administered alone at 10 mg·kg-1.
Lost beneficial effect when co-administered with 5.2 mg·kg-1 meclizine.
Maintained a statistically significant 15% reduction in normalized spontaneous nystagmus frequency compared to vehicle controls when co-administered with 6.2 mg·kg-1 methylprednisolone.
Caused no reported side effects in treated animals.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1164115-89-2
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Appearance Oil
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분자량 235.33
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화학식 C12H21N5
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Color Light brown to brown
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SMILES
CNC1CN(C2=NC(CC(C)C)=NC(N)=C2)C1
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Synonyms
SENS-111
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Pure form -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 100 mg/mL (424.94 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
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Data Sheet (273 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Petremann M, et al. Effect of the novel histamine H4 receptor antagonist SENS-111 on spontaneous nystagmus in a rat model of acute unilateral vestibular loss. Br J Pharmacol. 2020;177(3):623-633. [Content Brief]
[2]. Venail F, et al. Safety, tolerability, pharmacokinetics and pharmacokinetic-pharmacodynamic modelling of the novel H4 receptor inhibitor SENS-111 using a modified caloric test in healthy subjects. Br J Clin Pharmacol. 2018;84(12):2836-2848. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 4.2494 mL | 21.2468 mL | 42.4935 mL | 106.2338 mL |
| 5 mM | 0.8499 mL | 4.2494 mL | 8.4987 mL | 21.2468 mL | |
| 10 mM | 0.4249 mL | 2.1247 mL | 4.2494 mL | 10.6234 mL | |
| 15 mM | 0.2833 mL | 1.4165 mL | 2.8329 mL | 7.0823 mL | |
| 20 mM | 0.2125 mL | 1.0623 mL | 2.1247 mL | 5.3117 mL | |
| 25 mM | 0.1700 mL | 0.8499 mL | 1.6997 mL | 4.2494 mL | |
| 30 mM | 0.1416 mL | 0.7082 mL | 1.4165 mL | 3.5411 mL | |
| 40 mM | 0.1062 mL | 0.5312 mL | 1.0623 mL | 2.6558 mL | |
| 50 mM | 0.0850 mL | 0.4249 mL | 0.8499 mL | 2.1247 mL | |
| 60 mM | 0.0708 mL | 0.3541 mL | 0.7082 mL | 1.7706 mL | |
| 80 mM | 0.0531 mL | 0.2656 mL | 0.5312 mL | 1.3279 mL | |
| 100 mM | 0.0425 mL | 0.2125 mL | 0.4249 mL | 1.0623 mL |
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