GW3965 hydrochloride
Based on 29 publication(s) in Google Scholar
GW3965 hydrochloride is a potent and selective liver X receptor (LXR) agonist with EC50s of 190 nM and 30 nM for hLXRα and hLXRβ, respectively.
For research use only. We do not sell to patients.
- Purity: 99.96%
- CAS No.: 405911-17-3
- Formula: C33H32Cl2F3NO3
- Molecular Weight:618.51
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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Publications Citing Use of MedChemExpress (MCE) GW3965 hydrochloride
More- Nat Commun. 2025 Nov 6;16(1):9805. [Abstract]
- Theranostics. 2020 Jul 11;10(19):8834-8850. [Abstract]
- MedComm (2020). 2025 Sep 27;6(10):e70411. [Abstract]
- Sci Adv. 2022 Jul 15;8(28):eabn5295. [Abstract]
- Cell Death Differ. 2020 Aug;27(8):2433-2450. [Abstract]
- Environ Sci Technol. 2025 Apr 25. [Abstract]
- Cancer Lett. 2023 Jun 28:564:216208. [Abstract]
- Environ Int. 2026 Jul:213:110355. [Abstract]
- Environ Int. 2024 Nov 26:194:109168. [Abstract]
- J Transl Med. 2025 May 14;23(1):542. [Abstract]
- JHEP Rep. 2026 May 5.
- Brain Behav Immun. 2025 Aug 21:106089. [Abstract]
- Fundam Res. 2026 Mar 12.
- J Ethnopharmacol. 2026 Apr 6:360:121150. [Abstract]
- J Ethnopharmacol. 2023 Oct 28:315:116684. [Abstract]
- J Am Heart Assoc. 2021 May 18;10(10):e018455. [Abstract]
- Respir Res. 2024 Nov 7;25(1):399. [Abstract]
- Int Immunopharmacol. 2026 Jan 1;168(Pt 2):115878. [Abstract]
- Biogerontology. 2025 Jan 31;26(2):49. [Abstract]
- Bioconjug Chem. 2015 Nov 18;26(11):2216-22. [Abstract]
- Am J Physiol Endocrinol Metab. 2019 Jun 1;316(6):E1136-E1145. [Abstract]
- Viruses. 2022 Mar 3;14(3):514. [Abstract]
- Drug Metab Dispos. 2026 May 13. [Abstract]
- Cytokine. 2025 May 7:191:156955. [Abstract]
- Immun Inflamm Dis. 2025 Aug;13(8):e70243. [Abstract]
- Vet Microbiol. 2024 Jan:288:109948. [Abstract]
- SSRN. 2025 Aug 13.
- bioRxiv. 2023 Mar 10.
- Radboud University Nijmegen. 2021 Mar.
Customer Validation & Images
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Cell Imaging/Staining
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Others
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RT-PCR
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WB
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Cell Proliferation/Viability Assay
Biological Activity
EC50: 190 nM (hLXRα), 30 nM (hLXRβ)[4]
GW3965 hydrochloride promotes GBM cell death in vitro with enhanced efficacy in EGFRvIII-expressing tumor cells. GW3965 hydrochloride up-regulates expression of the cholesterol transporter gene ABCA1 and the E3 ubiquitin ligase IDOL and reduces LDLR levels[2]. LXR ligands inhibits platelet aggregation and calcium mobilization stimulated by collagen or CRP. GW3965 hydrochloride (1 or 5 μM) displays a minor inhibitory effect on fibrinogen binding and P-selectin exposure, when platelets are stimulated with 1 μg/mL CRP. But using higher concentrations of GW3965 hydrochloride (10 μM) or T0901317 (40 μM), the levels of fibrinogen and P-selectin on the platelet surface are reduced[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 405911-17-3
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Appearance Solid
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Molecular Weight 618.51
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Formula C33H32Cl2F3NO3
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Color White to off-white
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SMILES
ClC1=C(C(F)(F)F)C=CC=C1CN(CC(C2=CC=CC=C2)C3=CC=CC=C3)CCCOC4=CC(CC(O)=O)=CC=C4.[H]Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (29)
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Journal Impact Factor
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Most Recent
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Nat Commun
PROTAC repurposing uncovers a noncanonical binding surface that mediates chemical degradation of nuclear receptors. [Abstract]2025 Nov 6;16(1):9805. PMID: 41198675 -
Theranostics
LXR activation potentiates sorafenib sensitivity in HCC by activating microRNA-378a transcription. [Abstract]2020 Jul 11;10(19):8834-8850. PMID: 32754282
GW3965 hydrochloride purchased from MedChemExpress. Usage Cited in: Theranostics. 2020 Jul 11;10(19):8834-8850. [Abstract]
Flow cytometry showed the combination of sorafenib and GW3965 (1, 2 μM) could induce apoptosis in Huh7-SR and HCCLM3-SR.
GW3965 hydrochloride purchased from MedChemExpress. Usage Cited in: Theranostics. 2020 Jul 11;10(19):8834-8850. [Abstract]
Colony-formation efficiency showed the emergency of Huh7-SR coloines which treated with Sorafenib and GW3965 (1, 2 μM) was less than that treated with Sorafenib alone.
GW3965 hydrochloride purchased from MedChemExpress. Usage Cited in: Theranostics. 2020 Jul 11;10(19):8834-8850. [Abstract]
WB showed IGF1R were upregulated in combination along with their common downstream target pERK/p-AKT and combination treatment also could induce apoptosis treated with GW3965 (1, 2 μM).
GW3965 hydrochloride purchased from MedChemExpress. Usage Cited in: Theranostics. 2020 Jul 11;10(19):8834-8850. [Abstract]
The impact of Sorafenib, GW3965 and the combination therapy on cell viability in Huh7-SR and HCCLM3-SR cells were determined by CCK8 assay.
GW3965 hydrochloride purchased from MedChemExpress. Usage Cited in: Theranostics. 2020 Jul 11;10(19):8834-8850. [Abstract]
Immunohistochemistry showed Sorafenib and GW3965 (30 mg/kg) combination therapy could suppress HCC proliferation and IGF1R level in vivo.
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MedComm (2020)
Cholesterol 25-Hydroxylase Enhances Myeloid-Derived Suppressor Cell (MDSC) Immunosuppression via the Stimulator of Interferon Genes (STING)-Tank-Binding Kinase 1 (TBK1)-Receptor-Interacting Protein Kinase 3 (RIPK3) Pathway in Colorectal Cancer. [Abstract]2025 Sep 27;6(10):e70411. PMID: 41020041 -
Sci Adv
ZMYND8 is a master regulator of 27-hydroxycholesterol that promotes tumorigenicity of breast cancer stem cells. [Abstract]2022 Jul 15;8(28):eabn5295. PMID: 35857506 -
Cell Death Differ
The lipogenic LXR-SREBF1 signaling pathway controls cancer cell DNA repair and apoptosis and is a vulnerable point of malignant tumors for cancer therapy. [Abstract]2020 Aug;27(8):2433-2450. PMID: 32144382 -
Environ Sci Technol
Impact of 1,2-Bis (2,4,6-Tribromophenoxy) Ethane on Liver Metabolism and Intestinal Health in Zebrafish: Role of the Liver X Receptor. [Abstract]2025 Apr 25. PMID: 40277015 -
Cancer Lett
Myeloid-derived suppressor cells deficient in cholesterol biosynthesis promote tumor immune evasion. [Abstract]2023 Jun 28:564:216208. PMID: 37150500 -
Environ Int
Lipid metabolic disruption: A potential mechanistic pathway for 2,4,6-tribromophenol-induced neurotoxicity in zebrafish. [Abstract]2026 Jul:213:110355. PMID: 42288112 -
Environ Int
Cresyl diphenyl phosphate (a novel organophosphate ester) induces hepatic steatosis by directly binding to liver X receptor α: From molecule action to risk assessment. [Abstract]2024 Nov 26:194:109168. PMID: 39612745
GW3965 hydrochloride purchased from MedChemExpress. Usage Cited in: Environ Int. 2024 Nov 26:194:109168. [Abstract]
Representative images of Oil red O straining of HepG2 cells after treated with different concentrations of GW3965 (0, 1, and 10 μM; 72 h).
GW3965 hydrochloride purchased from MedChemExpress. Usage Cited in: Environ Int. 2024 Nov 26:194:109168. [Abstract]
Total triglycerides (TG) and total cholesterol (T-CHO) contents of HepG2 cells after treated with GW3965 (1-10 μM; 72 h).
GW3965 hydrochloride purchased from MedChemExpress. Usage Cited in: Environ Int. 2024 Nov 26:194:109168. [Abstract]
Expression of the genes in HepG2 cells measured by qRT-PCR after treated with GW3965 (1-10 μM).
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J Transl Med
Mitochondrial dysfunction fuels drug resistance in adult T-cell acute lymphoblastic leukemia. [Abstract]2025 May 14;23(1):542. PMID: 40369632
GW3965 hydrochloride purchased from MedChemExpress. Usage Cited in: J Transl Med. 2025 May 14;23(1):542. [Abstract]
Control or Ethidium Bromide treated (100-200 ng/mL; 7 d) CCRF-CEM and MOLT-4 cells, were treated with the indicated concentrations of GW3965 (0.5-10 μM; 24 h) and the accumulation of P-gp and β-actin was visualized as above.
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Brain Behav Immun
LXR-β regulates microglial efferocytosis and neuroinflammation in CPSP via STAT6 activation. [Abstract]2025 Aug 21:106089. PMID: 40848997 -
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J Ethnopharmacol
Xiaoyan Lidan formula ameliorates cholecystitis by regulating cholesterol transportation and water permeability of the gall bladder through the activation of LXRβ. [Abstract]2026 Apr 6:360:121150. PMID: 41485629 -
J Ethnopharmacol
QiShenYiQi pill inhibits atherosclerosis by promoting reverse cholesterol transport PPARγ-LXRα/β-ABCA1 pathway. [Abstract]2023 Oct 28:315:116684. PMID: 37230281 -
J Am Heart Assoc
Protective Functions of Liver X Receptor α in Established Vulnerable Plaques: Involvement of Regulating Endoplasmic Reticulum-Mediated Macrophage Apoptosis and Efferocytosis. [Abstract]2021 May 18;10(10):e018455. PMID: 33969692 -
Respir Res
Activation of LXR signaling ameliorates apoptosis of alveolar epithelial cells in Bronchopulmonary dysplasia. [Abstract]2024 Nov 7;25(1):399. PMID: 39511537
GW3965 hydrochloride purchased from MedChemExpress. Usage Cited in: Respir Res. 2024 Nov 7;25(1):399. [Abstract]
MLE12 cells were cultured under normoxia (NOX) or hyperoxia (HYX) conditions with different doses of GW3965 (1-10 μM) for 24 h, and cell viability was determined by CCK-8 assays.
GW3965 hydrochloride purchased from MedChemExpress. Usage Cited in: Respir Res. 2024 Nov 7;25(1):399. [Abstract]
MLE12 cells were cultured under normoxia (NOX) or hyperoxia (HYX) conditions with different doses of GW3965 (1-15 μM) for 24 h, and detected relative mRNA expression of Abca1 normalized to Gapdh.
GW3965 hydrochloride purchased from MedChemExpress. Usage Cited in: Respir Res. 2024 Nov 7;25(1):399. [Abstract]
Representative pictures of MLE12 cells exposed to NOX or HYX for 24 h treated with or without 5 µM GW3965 stained by Filipin III and the quantification of the mean fluorescence intensity of Filipin III staining.
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Int Immunopharmacol
Sirtuin 6 activator UBCS039 ameliorates hepatic lipogenesis through liver X receptor deacetylation. [Abstract]2026 Jan 1;168(Pt 2):115878. PMID: 41265217 -
Biogerontology
Upregulation of LXRβ/ABCA1 pathway alleviates cochlear hair cell senescence of C57BL/6 J mice via reducing lipid droplet accumulation. [Abstract]2025 Jan 31;26(2):49. PMID: 39890652 -
Bioconjug Chem
2015 Nov 18;26(11):2216-22. PMID: 25945727 -
Am J Physiol Endocrinol Metab
Liver X receptor-α activation enhances cholesterol secretion in lactating mammary epithelium. [Abstract]2019 Jun 1;316(6):E1136-E1145. PMID: 30964702 -
Viruses
2022 Mar 3;14(3):514. PMID: 35336921 -
Drug Metab Dispos
Synergistic hepatotoxicity of azithromycin and acetaminophen involves liver X receptor α-mediated metabolic dysregulation and endoplasmic reticulum stress. [Abstract]2026 May 13. PMID: 42263432 -
Cytokine
Eliminating myeloid-derived suppressor cells alleviates immunosuppression and reduces susceptibility to secondary infections in a two-hit sepsis model. [Abstract]2025 May 7:191:156955. PMID: 40339353 -
Immun Inflamm Dis
Liver X Receptor Activation Alleviates Hepatic Ischemia-Reperfusion Injury in Diabetes by Inhibiting NF-κB-NLRP3 Activation. [Abstract]2025 Aug;13(8):e70243. PMID: 40778489 -
Vet Microbiol
The activation of liver X receptors in Madin-Darby bovine kidney cells and mice restricts infection by bovine viral diarrhea virus. [Abstract]2024 Jan:288:109948. PMID: 38113573 -
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Solvent & Solubility
DMSO : 100 mg/mL (161.68 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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)
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 (4.04 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
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 (4.04 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: Corn Oil
Solubility: 10 mg/mL (16.17 mM); Suspended solution; Need ultrasonic
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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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.
Protocol
Cells are seeded in 96 wells and are treated after 24 hours with different drugs indicated in each experiment in medium containing 1% FBS or lipoprotein deficient serum. Relative proliferation is determined using Cell Proliferation Assay Kit. Cells are incubated 1.5 hrs after adding tetrazolium salt WST-1 [2-(4-iodophenyl)-3- (4-nitrophenyl)-5-(2, 4-disulfo-phenyl)-2H-tetrazolium, monosodium salt] at 5% CO2, 37ºC and the absorbance of the treated and untreated cells are measured using a microplate reader at 420 to 480 nm. Cells seeded in 12 well plates are counted using a hemocytometer, and dead cells are assessed using trypan blue exclusion assays.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Diabetes is induced in two-month-old male rats by a single i.p. injection of freshly prepared STZ (65 mg/kg) in 0.09 M citrate buffer, pH 4.8. Control animals are injected with 0.09 mol/L citrate buffer at pH 4.8. Hyperglycemia is confirmed 48 h after streptozotocin injection by measuring tail vein blood glucose levels using a glucometer OneTouch Ultra2. Only animals with mean plasma glucose levels over 300 mg/mL are classified as diabetic. Glycemia is also assessed before treatment with Ro5-4864 or GW3965 hydrochloride and before death. Two months after STZ injection, diabetic animals are treated once a week with Ro5-4864 (3 mg/kg) or GW3965 hydrochloride (50 mg/kg). Thus, they receive four subcutaneous injections in a month. Control diabetic rats receive 200 μL of vehicle (sesame oil). Four-month-old non-diabetic male rats are injected, following the same experimental schedule, with Ro5-4864, GW3965 hydrochloride or vehicle. Rats are killed 24 h after the last treatment.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (285 KB)
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SDS (476 KB)
- English - EN (476 KB)
- Français - FR (476 KB)
- Deutsch - DE (476 KB)
- Norwegian - NO (476 KB)
- Español - ES (476 KB)
- Swedish - SV (476 KB)
- Italian - IT (476 KB)
- Korean - KR (476 KB)
- Portuguese - PT (476 KB)
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Handling Instructions (2659 KB)
References
[1]. Mitro, Nico., et al. LXR and TSPO as new therapeutic targets to increase the levels of neuroactive steroids in the central nervous system of diabetic animals. Neurochemistry International (2012), 60(6), 616-621. [Content Brief]
[3]. Spyridon, Michael., et al. LXR as a novel antithrombotic target. Blood (2011), 117(21), 5751-5761. [Content Brief]
[4]. Collins JL, et al. Identification of a nonsteroidal liver X receptor agonist through parallel array synthesis of tertiary amines. J Med Chem. 2002 May 9;45(10):1963-6. [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 (sealed storage, away from moisture). 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 | 1.6168 mL | 8.0839 mL | 16.1679 mL | 40.4197 mL |
| 5 mM | 0.3234 mL | 1.6168 mL | 3.2336 mL | 8.0839 mL | |
| 10 mM | 0.1617 mL | 0.8084 mL | 1.6168 mL | 4.0420 mL | |
| 15 mM | 0.1078 mL | 0.5389 mL | 1.0779 mL | 2.6946 mL | |
| 20 mM | 0.0808 mL | 0.4042 mL | 0.8084 mL | 2.0210 mL | |
| 25 mM | 0.0647 mL | 0.3234 mL | 0.6467 mL | 1.6168 mL | |
| 30 mM | 0.0539 mL | 0.2695 mL | 0.5389 mL | 1.3473 mL | |
| 40 mM | 0.0404 mL | 0.2021 mL | 0.4042 mL | 1.0105 mL | |
| 50 mM | 0.0323 mL | 0.1617 mL | 0.3234 mL | 0.8084 mL | |
| 60 mM | 0.0269 mL | 0.1347 mL | 0.2695 mL | 0.6737 mL | |
| 80 mM | 0.0202 mL | 0.1010 mL | 0.2021 mL | 0.5052 mL | |
| 100 mM | 0.0162 mL | 0.0808 mL | 0.1617 mL | 0.4042 mL |
GW3965 hydrochloride Related Classifications
HY-10627A Related Classifications
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