2. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  3. Histamine Receptor
  4. Seliforant

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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Seliforant

Seliforant Chemical Structure

CAS No. : 1164115-89-2

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10 mM * 1 mL in DMSO
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Seliforant Related Antibodies

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Description

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[1][2].

IC50 & Target[1]

H4 receptor

 

In Vitro

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 Related Antibodies
In Vivo

Seliforant (SENS-111) (10-20 mg·kg-1; i.v.; single dose) at 10 mg·kg-1 (i.v.) produces a statistically significant 22% reduction in normalized spontaneous nystagmus frequency in Rattus norvegicus with acute unilateral vestibular loss at the peak of vertigo symptoms, while the 20 mg·kg-1 dose does not yield a significant effect[1].
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.

Animal Model: Long-Evans (12-week-old female, ~175-200 g, acute unilateral vestibular loss induced via two transtympanic injections of kainic acid)[1]
Dosage: 10 mg·kg-1; 20 mg·kg-1
Administration: i.v.; single dose
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.
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]
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
Administration: i.v.; single dose; i.p. (meclizine, methylprednisolone)
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.
Clinical Trial
Molecular Weight

235.33

Formula

C12H21N5
CAS No.
Appearance

Oil

Color

Light brown to brown

SMILES

CNC1CN(C2=NC(CC(C)C)=NC(N)=C2)C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Pure form -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.2494 mL 21.2468 mL 42.4935 mL
5 mM 0.8499 mL 4.2494 mL 8.4987 mL
View the 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.

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Purity & Documentation
References

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
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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Seliforant Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Seliforant1164115-89-2SENS-111SENS111SENS 111Histamine Receptorspontaneous nystagmusblood-brain barriermethylprednisoloneratshistamine H4 receptorexcitotoxic acute unilateral vestibular lossmeclizinevestibular disordersvestibular neuronvertigoInhibitorinhibitorinhibit

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