Safotibant
Based on 1 Customer Validation
Safotibant (LF22-0542) is a selective antagonist for kinin B1 receptor (BKB1R), with Ki of 0.35 and 6.5 nM, for human and mouse BKB1R, respectively. Safotibant exhibits analgesic and anti-inflammatory property in mice model.
For research use only. We do not sell to patients.
- Purity : 98.88%
- CAS No.: 633698-99-4
- Formula: C25H34N4O5S
- Molecular Weight:502.63
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Storage:Pure form -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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![Sar-[D-Phe8]-des-Arg9-Bradykinin](https://file.medchemexpress.com/product_pic/hy-103291.gif)
HY-103291
Sar-[D-Phe8]-des-Arg9-BradykininB1 Receptor Agonist
All Bradykinin Receptor Isoforms
More
Biological Activity
Description
In Vivo
Safotibant (one eye drop application, twice a day for 7 days) inhibits expressions of inflammatory mediators B1R, iNOS, IL-1β, COX-2, VEGF-R2 and HIF-1α, reverses diabetes-induced retinal inflammation and oxidative stress in streptozotocin (STZ)-diabetic Wistar rats model[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Osteolytic sarcoma xenograft C3H/HeJ mice model[1]
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Dosage:10 mg/kg
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Administration:s.c., 3 times a day for 8 days
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Result:Decreased numbers of flinching and time spent on spontaneous guarding.
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Animal Model:Streptozotocin (STZ)-diabetic Wistar rats model[2]
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Dosage:One eye drop
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Administration:On eyes application, twice a day for 7 days
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Result:Reversed retinal vascular hyperpermeability, decreased levels of retinal leukostasis and superoxide anion in 3 retinal nuclear layers.
Chemical Information
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CAS No. 633698-99-4
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Appearance Oil
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Molecular Weight 502.63
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Formula C25H34N4O5S
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Color White to light yellow
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SMILES
O=C(COCCN(S(=O)(C1=C(C)C=C(OC)C=C1C)=O)C)N(CC2=CC=C(C3=NCCN3)C=C2)C
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Synonyms
LF22-0542
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Shipping
Room temperature in continental US; may vary elsewhere.
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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 : 10 mg/mL (19.90 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)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1 mg/mL (1.99 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1 mg/mL (1.99 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (273 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
References
[1]. Sevcik MA, et al., Analgesic efficacy of bradykinin B1 antagonists in a murine bone cancer pain model. J Pain. 2005 Nov;6(11):771-5. [Content Brief]
[2]. Pouliot M, et al., Ocular application of the kinin B1 receptor antagonist LF22-0542 inhibits retinal inflammation and oxidative stress in streptozotocin-diabetic rats. PLoS One. 2012;7(3):e33864. [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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9895 mL | 9.9477 mL | 19.8954 mL | 49.7384 mL |
| 5 mM | 0.3979 mL | 1.9895 mL | 3.9791 mL | 9.9477 mL | |
| 10 mM | 0.1990 mL | 0.9948 mL | 1.9895 mL | 4.9738 mL | |
| 15 mM | 0.1326 mL | 0.6632 mL | 1.3264 mL | 3.3159 mL |
Safotibant Related Classifications
HY-100827 Related Classifications
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