Elexacaftor
Based on 51 publication(s) in Google Scholar
Elexacaftor (VX-445, Compound 1) is a modulator of cystic fibrosis transmembrane conductance regulator (CFTR). Elexacaftor (VX-445, Compound 1) facilitates the processing and trafficking of CFTR to increase the amount of CFTR at the cell surface.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 99.26%
- CAS No.: 2216712-66-0
- 화학식: C26H34F3N7O4S
- 분자량:597.65
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) Elexacaftor
More- Am J Respir Crit Care Med. 2021 Nov 15;204(10):1231-1235. [Abstract]
- J Clin Invest. 2024 Jul 2:e176328. [Abstract]
- J Clin Invest. 2021 Aug 16;131(16):e150398. [Abstract]
- Mol Ther. 2026 Jul 1;34(7):4212-4225. [Abstract]
- Br J Pharmacol. 2025 Aug 20. [Abstract]
- J Med Chem. 2024 Aug 22;67(16):13891-13908. [Abstract]
- JCI Insight. 2026 Mar 23;11(6):e198846. [Abstract]
- JCI Insight. 2020 Sep 17;5(18):e139983. [Abstract]
- J Cyst Fibros. 2026 Jun 4:S1569-1993(26)01638-3. [Abstract]
- J Cyst Fibros. 2026 Jun 16:S1569-1993(26)01643-7. [Abstract]
- J Cyst Fibros. 2025 May;24(3):552-561. [Abstract]
- J Cyst Fibros. 2025 Jan;24(1):164-174. [Abstract]
- J Cyst Fibros. 2023 May;22(3):525-537. [Abstract]
- J Cyst Fibros. 2021 May;20(3):452-459. [Abstract]
- Am J Respir Cell Mol Biol. 2025 Mar;72(3):308-319. [Abstract]
- Cells. 2022 Dec 16;11(24):4096. [Abstract]
- Int J Mol Sci. 2026 Feb 23;27(4):2063. [Abstract]
- Int J Mol Sci. 2025 May 31;26(11):5306. [Abstract]
- Int J Mol Sci. 2023 Sep 26;24(19):14539. [Abstract]
- Int J Mol Sci. 2023 Jun 19;24(12):10358. [Abstract]
- Int J Mol Sci. 2021 Dec 21;23(1):24. [Abstract]
- Int J Mol Sci. 2021 Mar 17;22(6):3063. [Abstract]
- Am J Physiol Cell Physiol. 2025 Oct 1;329(4):C1130-C1138. [Abstract]
- Am J Physiol Cell Physiol. 2022 Oct 1;323(4):C1215-C1230. [Abstract]
- Am J Physiol Cell Physiol. 2020 Aug 1;319(2):C331-C344. [Abstract]
- J Physiol. 2025 May;603(9):2619-2632. [Abstract]
- Structure. 2022 Aug 4;30(8):1190-1207.e5. [Abstract]
- iScience. 2024 Aug 9;27(9):110703. [Abstract]
- iScience. 2023 Oct 12;26(11):108180. [Abstract]
- Hum Gene Ther. 2024 Sep;35(17-18):695-709. [Abstract]
- J Biol Chem. 2024 Nov;300(11):107873. [Abstract]
- Microbiol Spectr. 2025 Sep 2;13(9):e0227524. [Abstract]
- PNAS Nexus. 2025 Jul 4;4(7):pgaf211. [Abstract]
- J Cell Sci. 2022 Mar 1;135(5):jcs259002. [Abstract]
- Orphanet J Rare Dis. 2024 Sep 13;19(1):343. [Abstract]
- Front Physiol. 2021 Feb 4;12:619442. [Abstract]
- Respir Med. 2025 Dec:250:108478. [Abstract]
- Glycoconj J. 2025 Feb;42(1):1-14. [Abstract]
- PLoS One. 2025 Sep 16;20(9):e0330974. [Abstract]
- Respir Investig. 2024 Mar 27;62(3):455-461. [Abstract]
- STAR Protoc. 2023 Jun 12;4(3):102337. [Abstract]
- University of Lisbon. 2026.
- J Pers Med. 2026 Jan 15;16(1):51. [Abstract]
- bioRxiv. 2025 April 11.
- bioRxiv. 2025 February 27.
- bioRxiv. 2025 Nov 14:2024.10.30.620903. [Abstract]
- bioRxiv. 2024 October 17.
- bioRxiv. 2024 August 16.
- University of Kentucky. 2022 Aug.
- J Pers Med. 2022 Apr 14;12(4):632. [Abstract]
- J Pers Med. 2020 Nov 5;10(4):209. [Abstract]
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Others
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Bio/Physico-chemical Assay
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Bio/Physico-chemical Assay
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WB
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WB
Biological Activity
CFTR[1].
Elexacaftor (VX-445) is a next-generation cystic fibrosis transmembrane conductance regulator (CFTR) corrector designed to restore Phe508del CFTR protein function. Elexacaftor (VX-445) has the potential to treat cystic fibrosis. VX-445-Tezacaftor-VX-770 significantly improves Phe508del CFTR protein processing, trafficking, and chloride transport to a greater extent than any two of these agents in dual combination[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2216712-66-0
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Appearance Solid
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분자량 597.65
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화학식 C26H34F3N7O4S
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Color White to off-white
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SMILES
CC1(C)C[C@H](C)CN1C2=C(C(NS(C3=CN(C)N=C3C)(=O)=O)=O)C=CC(N4C=CC(OCC(C)(C(F)(F)F)C)=N4)=N2
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Synonyms
VX-445
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (51)
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Journal Impact Factor
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Most Recent
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Am J Respir Crit Care Med
Elexacaftor/Tezacaftor/Ivacaftor Improved Clinical Outcomes in a Patient with N1303K-CFTR Based on In Vitro Experimental Evidence. [Abstract]2021 Nov 15;204(10):1231-1235. PMID: 34379998
Elexacaftor purchased from MedChemExpress. Usage Cited in: Am J Respir Crit Care Med. 2021 Nov 15;204(10):1231-1235. [Abstract]
Western blot of CFTR variances transiently expressed in HEK293 (left) or CFBE (right) cells. Cells were transfected with indicated CFTR variances overnight and then treated with VX445 (Elexacaftor: 2 μM) /VX661 or DMSO for 24 hours.
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J Clin Invest
Potentiation of BKCa channels by cystic fibrosis transmembrane conductance regulator (CFTR) correctors VX-445 and VX-121. [Abstract]2024 Jul 2:e176328. PMID: 38954478
Elexacaftor purchased from MedChemExpress. Usage Cited in: J Clin Invest. 2024 Jul 2:e176328. [Abstract]
Subsequent to amiloride, short-circuit current (Isc) was increased by the C2 CFTR correctors VX-445 (10 μM).
Elexacaftor purchased from MedChemExpress. Usage Cited in: J Clin Invest. 2024 Jul 2:e176328. [Abstract]
Recording of force in millinewtons (mN) over time from a single mesenteric artery showing preconstriction with the prostaglandin mimetic U46619 (1 × 10−7 to 5 × 10−7 M), after which the ability of increasing concentrations of VX-445 (Elexacaftor) to induce vasorelaxation was assessed. We added 0 Ca2+ at the end to determine maximal vasorelaxation.
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J Clin Invest
Inflammatory cytokines TNF-α and IL-17 enhance the efficacy of cystic fibrosis transmembrane conductance regulator modulators. [Abstract]2021 Aug 16;131(16):e150398. PMID: 34166230
Elexacaftor purchased from MedChemExpress. Usage Cited in: J Clin Invest. 2021 Aug 16;131(16):e150398. [Abstract]
Human airway epithelia from CFTR-ΔF508 donors were treated for 48 hours with a combination of elexacaftor (3 μM), tezacaftor (18 μM), and ivacaftor (1 μM), either alone or in the presence of TNF-α+IL-17. pHASL was measured using SNARF-1-dextran.
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Mol Ther
2026 Jul 1;34(7):4212-4225. PMID: 41925277 -
Br J Pharmacol
In silico, in vitro and ex vivo characterization of cystic fibrosis transmembrane conductance regulator pathogenic variants localized in the fourth intracellular loop and their rescue by modulators. [Abstract]2025 Aug 20. PMID: 40831301 -
J Med Chem
Synthesis and Biological Evaluation of Pyrazole-Pyrimidones as a New Class of Correctors of the Cystic Fibrosis Transmembrane Conductance Regulator (CFTR). [Abstract]2024 Aug 22;67(16):13891-13908. PMID: 39137389 -
JCI Insight
Targeting PI3Kγ anchoring enhances CFTR membrane localization and modulator efficacy via PKD1. [Abstract]2026 Mar 23;11(6):e198846. PMID: 41869727
Elexacaftor purchased from MedChemExpress. Usage Cited in: JCI Insight. 2026 Mar 23;11(6):e198846. [Abstract]
Representative immunogold electron microscopy images showing the distribution of overexpressed F508del-CFTR-GFP in HEK293T cells. Cells were treated for 24 hours with DMSO (Veh), ETI (3 μM VX-445, 10 μM VX-661, and 1 μM VX-770) plus control peptide (ETI + 25 μM CP), or ETI plus PI3Kγ MP (ETI + 25 μM PI3Kγ MP). HEK293T cells expressing WT CFTR-GFP served as positive controls.
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JCI Insight
Allosteric folding correction of F508del and rare CFTR mutants by elexacaftor-tezacaftor-ivacaftor (Trikafta) combination. [Abstract]2020 Sep 17;5(18):e139983. PMID: 32853178 -
J Cyst Fibros
Vanzacaftor-Tezacaftor as an alternative therapeutic resource for the ETI-Resistant L467F-F508del Allele: Ex vivo prediction and exploratory clinical assessment. [Abstract]2026 Jun 4:S1569-1993(26)01638-3. PMID: 42243036 -
J Cyst Fibros
A functional comparison of vanzacaftor/tezacaftor/deutivacaftor and elexacaftor/tezacaftor/ivacaftor in patient-derived intestinal organoids with rare CFTR variants. [Abstract]2026 Jun 16:S1569-1993(26)01643-7. PMID: 42303492 -
J Cyst Fibros
Evaluation of the response to elexacaftor-tezacaftor-ivacaftor of the rare CFTR variants L383S, I507del, L1065P and R1066H in intestinal organoid-derived epithelial monolayers. [Abstract]2025 May;24(3):552-561. PMID: 39979195 -
J Cyst Fibros
A W1282X cystic fibrosis mouse allows the study of pharmacological and gene-editing therapeutics to restore CFTR function. [Abstract]2025 Jan;24(1):164-174. PMID: 39532588 -
J Cyst Fibros
Rescue by elexacaftor-tezacaftor-ivacaftor of the G1244E cystic fibrosis mutation's stability and gating defects are dependent on cell background. [Abstract]2023 May;22(3):525-537. PMID: 36543707
Elexacaftor purchased from MedChemExpress. Usage Cited in: J Cyst Fibros. 2023 May;22(3):525-537. [Abstract]
Elexacaftor/Tezacaftor (elexa/teza; 3 μM/10 μM; 24 h) combination causes a significant increase in the expression of the mature protein, with no changes in the expression of the immature, core-glycosylated form (B band) in Epithelia.
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J Cyst Fibros
2021 May;20(3):452-459. PMID: 32674984 -
Am J Respir Cell Mol Biol
Distinct Responses of Cystic Fibrosis Epithelial Cells to SARS-CoV-2 and Influenza A Virus. [Abstract]2025 Mar;72(3):308-319. PMID: 39311876 -
Cells
2022 Dec 16;11(24):4096. PMID: 36552859 -
Int J Mol Sci
Restoration of Defective CFTR in Human Nasal Respiratory Epithelial Cells by CFTR Modulators and mRNA Transfection. [Abstract]2026 Feb 23;27(4):2063. PMID: 41752197 -
Int J Mol Sci
2025 May 31;26(11):5306. PMID: 40508114 -
Int J Mol Sci
CFTR Function Restoration upon Elexacaftor/Tezacaftor/Ivacaftor Treatment in Patient-Derived Intestinal Organoids with Rare CFTR Genotypes. [Abstract]2023 Sep 26;24(19):14539. PMID: 37833986 -
Int J Mol Sci
Theratyping of the Rare CFTR Genotype A559T in Rectal Organoids and Nasal Cells Reveals a Relevant Response to Elexacaftor (VX-445) and Tezacaftor (VX-661) Combination. [Abstract]2023 Jun 19;24(12):10358. PMID: 37373505 -
Int J Mol Sci
Rare Trafficking CFTR Mutations Involve Distinct Cellular Retention Machineries and Require Different Rescuing Strategies. [Abstract]2021 Dec 21;23(1):24. PMID: 35008443 -
Int J Mol Sci
2021 Mar 17;22(6):3063. PMID: 33802742 -
Am J Physiol Cell Physiol
(R)-vanzacaftor potentiates BKCa channels in the absence of CFTR correction or potentiation. [Abstract]2025 Oct 1;329(4):C1130-C1138. PMID: 40920663 -
Am J Physiol Cell Physiol
KCa3.1 potentiation stimulates Cl- secretion in F508del and G551D CFTR-corrected primary human bronchial epithelial cells. [Abstract]2022 Oct 1;323(4):C1215-C1230. PMID: 36062876 -
Am J Physiol Cell Physiol
2020 Aug 1;319(2):C331-C344. PMID: 32432926 -
J Physiol
2025 May;603(9):2619-2632. PMID: 40047394 -
Structure
Triangulating variation in the population to define mechanisms for precision management of genetic disease. [Abstract]2022 Aug 4;30(8):1190-1207.e5. PMID: 35714602 -
iScience
Defective CFTR modulates mechanosensitive channels TRPV4 and PIEZO1 and drives endothelial barrier failure. [Abstract]2024 Aug 9;27(9):110703. PMID: 39252977 -
iScience
In silico analysis and theratyping of an ultra-rare CFTR genotype (W57G/A234D) in primary human rectal and nasal epithelial cells. [Abstract]2023 Oct 12;26(11):108180. PMID: 38026150 -
Hum Gene Ther
SP-101, A Novel Adeno-Associated Virus Gene Therapy for the Treatment of Cystic Fibrosis, Mediates Functional Correction of Primary Human Airway Epithelia From Donors with Cystic Fibrosis. [Abstract]2024 Sep;35(17-18):695-709. PMID: 39155805 -
J Biol Chem
A nonnatural peptide targeting the A-kinase anchoring function of PI3Kγ for therapeutic cAMP modulation in pulmonary cells. [Abstract]2024 Nov;300(11):107873. PMID: 39393573 -
Microbiol Spectr
Condition-dependent effects of Elexacaftor/Tezacaftor/Ivacaftor (Trikafta) on Aspergillus fumigatus growth. [Abstract]2025 Sep 2;13(9):e0227524. PMID: 40736245 -
PNAS Nexus
VX-445 (elexacaftor) inhibits chloride secretion across human bronchial epithelial cells by directly blocking KCa3.1 channels. [Abstract]2025 Jul 4;4(7):pgaf211. PMID: 40688096 -
J Cell Sci
Lipid-driven CFTR clustering is impaired in cystic fibrosis and restored by corrector drugs. [Abstract]2022 Mar 1;135(5):jcs259002. PMID: 35060604 -
Orphanet J Rare Dis
CFTR modulators response of S737F and T465N CFTR variants on patient-derived rectal organoids. [Abstract]2024 Sep 13;19(1):343. PMID: 39272186 -
Front Physiol
CFTR Correctors and Antioxidants Partially Normalize Lipid Imbalance but not Abnormal Basal Inflammatory Cytokine Profile in CF Bronchial Epithelial Cells. [Abstract]2021 Feb 4;12:619442. PMID: 33613309 -
Respir Med
Theratyping as a tool to guide clinical decision-making in patients with suspected cystic fibrosis and variants currently ineligible for CFTR modulator therapy. [Abstract]2025 Dec:250:108478. PMID: 41241150 -
Glycoconj J
Effect of CFTR modulators Elexacaftor/Tezacaftor/Ivacaftor on lipid metabolism in human bronchial epithelial cells. [Abstract]2025 Feb;42(1):1-14. PMID: 39797966 -
PLoS One
Alternative splicing and residual function potentially expand the therapeutic landscape of the CFTRdele2ins182 variant. [Abstract]2025 Sep 16;20(9):e0330974. PMID: 40956828 -
Respir Investig
Functional rescue of CFTR in rectal organoids from patients carrying R334W variant by CFTR modulators and PDE4 inhibitor Roflumilast. [Abstract]2024 Mar 27;62(3):455-461. PMID: 38547757 -
STAR Protoc
Protocol for generating airway organoids from 2D air liquid interface-differentiated nasal epithelia for use in a functional CFTR assay. [Abstract]2023 Jun 12;4(3):102337. PMID: 37314920 -
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J Pers Med
Functional, Cohort-Level Assessment of CFTR Modulator Responses Using Biobanked Nasal Epithelial Cells from Individuals with Cystic Fibrosis. [Abstract]2026 Jan 15;16(1):51. PMID: 41590543 -
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bioRxiv
Chronic pancreatitis patient-derived organoids reveal new paths to precision therapeutics. [Abstract]2025 Nov 14:2024.10.30.620903. PMID: 41279927 -
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J Pers Med
Theratyping of the Rare CFTR Variants E193K and R334W in Rectal Organoid-Derived Epithelial Monolayers. [Abstract]2022 Apr 14;12(4):632. PMID: 35455747 -
J Pers Med
Preclinical Studies of a Rare CF-Causing Mutation in the Second Nucleotide Binding Domain (c.3700A>G) Show Robust Functional Rescue in Primary Nasal Cultures by Novel CFTR Modulators. [Abstract]2020 Nov 5;10(4):209. PMID: 33167369
용액&용해도
DMSO : 125 mg/mL (209.15 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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: ≥ 2.08 mg/mL (3.48 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
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.
순도&문서
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Data Sheet (278 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.6732 mL | 8.3661 mL | 16.7322 mL | 41.8305 mL |
| 5 mM | 0.3346 mL | 1.6732 mL | 3.3464 mL | 8.3661 mL | |
| 10 mM | 0.1673 mL | 0.8366 mL | 1.6732 mL | 4.1831 mL | |
| 15 mM | 0.1115 mL | 0.5577 mL | 1.1155 mL | 2.7887 mL | |
| 20 mM | 0.0837 mL | 0.4183 mL | 0.8366 mL | 2.0915 mL | |
| 25 mM | 0.0669 mL | 0.3346 mL | 0.6693 mL | 1.6732 mL | |
| 30 mM | 0.0558 mL | 0.2789 mL | 0.5577 mL | 1.3944 mL | |
| 40 mM | 0.0418 mL | 0.2092 mL | 0.4183 mL | 1.0458 mL | |
| 50 mM | 0.0335 mL | 0.1673 mL | 0.3346 mL | 0.8366 mL | |
| 60 mM | 0.0279 mL | 0.1394 mL | 0.2789 mL | 0.6972 mL | |
| 80 mM | 0.0209 mL | 0.1046 mL | 0.2092 mL | 0.5229 mL | |
| 100 mM | 0.0167 mL | 0.0837 mL | 0.1673 mL | 0.4183 mL |