GBT1118
Based on 1 publication(s) in Google Scholar
GBT1118 is a potent and orally active allosteric modifier of hemoglobin oxygen affinity. GBT1118 increases tolerance to severe hypoxia.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.97%
- CAS. Nr.: 1628799-51-8
- Formel: C19H20N2O4
- Molecular Weight:340.37
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
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Publications Citing Use of MedChemExpress (MCE) GBT1118
More
Biologische Aktivität
GBT1118 binds covalently and reversibly via an imine intermediate to the N-terminal valine of hemoglobin α chain, and allosterically increases intracellular hemoglobin affinity for O2[1].
GBT1118 (25% of sample hemoglobin concentration) protects red blood cells from damage during severe hypoxia[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Blood and plasma pharmacokinetic parameters of GBT1118 in male mice following 10 mg/kg IV Administration of GBT1118[1]
| Matrix | T1/2 (h) | AUC0-∞ (μg⋅h/mL) | Vss (L/kg) | CLs (mL/min/kg) | Blood/Plasma Ratio |
| Blood | 13.9 | 2929 | 0.07 | 0.06 | 51.4 |
| Plasma | 11.3 | 60 | 2.95 | 3.21 |
Blood and plasma pharmacokinetic parameters of GBT1118 in male mice following 100 mg/kg PO Administration of GBT1118[1]
| Matrix | Tmax (h) | Cmax (μg/mL) | AUC0-∞ (μg•h/mL) | F (%) | Blood/Plasma Ratio |
| Blood | 2 | 318 | 13428 | 45.8 | 34.1 |
| Plasma | 8 | 12 | 224 | 33.5 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57Bl/6 mice, acute hypoxia model[1]
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Dosage:70 or 140 mg/kg
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Administration:Oral, single dose
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Result:Improved tolerance to 5% O2 hypoxia exposure. Increased O2 delivery during hypoxia, thus preserving MAP, HR, blood flow, and aerobic metabolism. Increased blood O2 loading in the lungs and allowed for increased O2 delivery during hypoxia. Decreased hypoxia in vital tissues and lowered lactate levels.
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Animal Model:C57Bl/6 mice[1]
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Dosage:10 or 100 mg/kg
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Administration:IV or PO (Pharmacokinetic Analysis)
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Result:Showed good pharmacokinetic parameters.
Chemical Information
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CAS. Nr. 1628799-51-8
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Appearance Solid
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Molecular Weight 340.37
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Formel C19H20N2O4
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Color White to off-white
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SMILES
O=C(C1=CN=CC=C1)N2[C@@H](CCCC2)COC3=C(C(O)=CC=C3)C=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Anal Bioanal Chem
Comprehensive metabolic characterization of GBT1118 in humans using a combined approach via UHPLC-HRMS for doping control. [Abstract]2026 Jun;418(12):3749-3761. PMID: 41963703
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (293.80 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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: 2.5 mg/mL (7.34 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: 2.5 mg/mL (7.34 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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.
Reinheit & Dokumentation
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Data Sheet (281 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)
Verweise
[1]. Dufu K, et al. GBT1118, a potent allosteric modifier of hemoglobin O2 affinity, increases tolerance to severe hypoxia in mice. Am J Physiol Heart Circ Physiol. 2017 Aug 1;313(2):H381-H391. [Content Brief]
[2]. Tarasev M, et al. GBT1118, a voxelotor analog, protects red blood cells from damage during severe hypoxia. Am J Transl Res. 2022 Jan 15;14(1):240-251. [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 | 2.9380 mL | 14.6899 mL | 29.3798 mL | 73.4495 mL |
| 5 mM | 0.5876 mL | 2.9380 mL | 5.8760 mL | 14.6899 mL | |
| 10 mM | 0.2938 mL | 1.4690 mL | 2.9380 mL | 7.3449 mL | |
| 15 mM | 0.1959 mL | 0.9793 mL | 1.9587 mL | 4.8966 mL | |
| 20 mM | 0.1469 mL | 0.7345 mL | 1.4690 mL | 3.6725 mL | |
| 25 mM | 0.1175 mL | 0.5876 mL | 1.1752 mL | 2.9380 mL | |
| 30 mM | 0.0979 mL | 0.4897 mL | 0.9793 mL | 2.4483 mL | |
| 40 mM | 0.0734 mL | 0.3672 mL | 0.7345 mL | 1.8362 mL | |
| 50 mM | 0.0588 mL | 0.2938 mL | 0.5876 mL | 1.4690 mL | |
| 60 mM | 0.0490 mL | 0.2448 mL | 0.4897 mL | 1.2242 mL | |
| 80 mM | 0.0367 mL | 0.1836 mL | 0.3672 mL | 0.9181 mL | |
| 100 mM | 0.0294 mL | 0.1469 mL | 0.2938 mL | 0.7345 mL |
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