Basimglurant
Based on 1 publication(s) in Google Scholar
Basimglurant (RG7090; RO4917523) is a selective, orally active, blood-brain barrier permeable negative allosteric modulator of metabotropic glutamate receptor 5 (mGluR5), with a Ki of 1.4 nM (against [3H]-ABP688 (HY-110141)) and 35.6 nM (against [3H]-MPEP (HY-14609A)). Basimglurant inhibits mGlu5-mediated signaling pathways and receptor constitutive activity, regulates dopamine levels in the nucleus accumbens, exerts anxiolytic, antidepressant-like, analgesic and arousal-promoting effects, and alters δ-wave power during non-rapid eye movement sleep. Basimglurant can be used in research on depression, fragile X syndrome, anxiety disorders, etc.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 98.0%
- CAS No.: 802906-73-6
- 화학식: C18H13ClFN3
- 분자량:325.77
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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용액&용해도
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- References
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Publications Citing Use of MedChemExpress (MCE) Basimglurant
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Biological Activity
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mGlu5 Receptor 1.1 nM (Kd) |
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Cell Line
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Type | Value | Description | References |
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| HEK293 | IC50 |
7 nM
Compound: 2
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Negative allosteric modulation of mGlu5 (unknown origin) expressed in HEK293 cells assessed as inhibition of L-AP4-induced calcium mobilization incubated for 30 mins prior to L-AP4 induction by Fluo-4 AM staining-based fluorescence assay
Negative allosteric modulation of mGlu5 (unknown origin) expressed in HEK293 cells assessed as inhibition of L-AP4-induced calcium mobilization incubated for 30 mins prior to L-AP4 induction by Fluo-4 AM staining-based fluorescence assay
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[PMID: 25565255] |
Basimglurant shows low metabolic stability in rat liver microsomes (11 μL/min/mg) and good stability in human liver microsomes (CL <10 μL/min/mg)[1].
Basimglurant shows no teratogenic potential in embryonic stem cell assays[1].
Basimglurant potently inhibits the binding of [3H]-MPEP to human, mouse and rat mGlu5 receptors, with Ki values of 35.6 nM, 29.5 nM and 33.2 nM for the three receptors, respectively[2].
Basimglurant potently inhibits Quisqualate-induced calcium mobilization in human, mouse, and rat mGlu5-expressing HEK293 cells, with IC50 values of 7.0 nM, 8.88 nM, and 7.48 nM, respectively[2].
Basimglurant potently inhibits Quisqualate-induced IP accumulation in HEK293 cells expressing human, mouse, and rat mGlu5, with IC50 values of 5.85 nM, 4.98 nM, and 5.93 nM, respectively. It also acts as an inverse agonist of the human mGlu5 receptor, with a corresponding IC50 of 38.1 nM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Basimglurant (10-30 mg/kg; p.o.; administered three times within 24 h) exerts antidepressant-like effects in the forced swimming test in rats[2].
Basimglurant (1-30 mg/kg; p.o.; single administration) induces a brain activity pattern highly similar to that of typical antidepressants in rats[2].
Basimglurant (0.03-0.3 mg/kg; p.o.; single administration) exhibits anxiolytic-like activity in the rat Vogel conflict test[2].
Basimglurant (0.01-1 mg/kg; p.o.; single administration) exerts anxiolytic effects in a mouse model of stress-induced hyperthermia[2].
Basimglurant (0.3-1 mg/kg; p.o.; single administration) exhibits anxiolytic-like activity in the rat conditioned emotional response test[2].
Basimglurant (0.1-1 mg/kg; p.o.; single administration) produces anxiolytic-like effects in the fear-potentiated startle test in rats[2].
Basimglurant (10 mg/kg; p.o.; single administration) exhibits analgesic activity in the late phase of the formalin-induced pain model in mice[2].
Basimglurant (0.1-10 mg/kg; subcutaneous injection; single administration) dose-dependently inhibits cold allodynia in rats with sciatic nerve ligation[2].
Basimglurant (0.03-0.3 mg/kg; intravenous administration; single dose) dose-dependently increases the micturition threshold volume in anesthetized rats[2].
Basimglurant (0.01-0.03 mg/kg; intravenous injection; single administration) potently reduces the bladder contraction frequency in anesthetized rats[2].
Basimglurant (0.03-0.3 mg/kg; p.o.; once daily; for 5 consecutive days) exerts a dose-dependent arousal-promoting effect during the active dark phase of Norwegian rats, reduces rapid eye movement (REM) sleep and non-rapid eye movement (non-REM) sleep, prolongs sleep latency, and enhances the δ-wave power of non-REM sleep[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wistar rats (male, 350 g, chronic mild stress-induced anhedonia model with unilateral ventral tegmental area electrode implantation)[2]
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Dosage:1 mg/kg; 3 mg/kg
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Administration:i.p.; daily; 21 days
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Result:Reduced the anhedonia index by -72% (day 35), -53% (day 39), and -64% (day 42) compared to vehicle-treated stressed rats at 3 mg/kg, normalizing values to pre-stress baseline levels.
Reduced the anhedonia index significantly with consistent effects across the treatment period at 1 mg/kg.
Had no significant effect on anhedonia index in unstressed rats.
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Animal Model:Wistar rats (male, 350 g, chronic mild stress-induced anhedonia model with unilateral ventral tegmental area electrode implantation)[2]
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Dosage:1 mg/kg; 3 mg/kg
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Administration:i.p.; daily; 21 days
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Result:Reduced the anhedonia index by -72% (day 35), -53% (day 39), and -64% (day 42) compared to vehicle-treated stressed rats at 3 mg/kg, normalizing values to pre-stress baseline levels.
Reduced the anhedonia index significantly with consistent effects across the treatment period at 1 mg/kg.
Had no significant effect on anhedonia index in unstressed rats.
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Animal Model:Sprague Dawley rats (male, 190-210 g, Vogel conflict drinking test model)[2]
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Dosage:0.03 mg/kg; 0.1 mg/kg; 0.3 mg/kg
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Administration:p.o.; single dose; 1 hour pre-test
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Result:Increased punished drinking time by +165% at 0.03 mg/kg, with further increases at higher doses, reaching significance at all tested doses compared to vehicle.
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Animal Model:Fischer F344 rats (male, ~250 g, fMRI-based brain activity profiling model)[2]
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Dosage:1 mg/kg; 10 mg/kg; 30 mg/kg
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Administration:p.o.; single dose; 1 hour pre-fMRI imaging
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Result:Increased perfusion in the dorsal striatum and decreased perfusion in the medial prefrontal cortex, dorsal hippocampus, thalamus, hypothalamus, septum, nucleus accumbens, ventral pallidum, and entorhinal piriform cortex at 1 mg/kg.
Amplified the perfusion changes observed at 1 mg/kg at 10 mg/kg.
Showed a pattern match coefficient (PMC) of >0.71 compared to prototypical antidepressants including duloxetine, reboxetine, imipramine, bupropion, and electroconvulsive treatment (ECT) at 1 and 10 mg/kg.
Surpassed the root mean square (RMS) response strength of ECT and standard antidepressants at 30 mg/kg at 1 and 10 mg/kg.
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Animal Model:Sprague Dawley rats (male, 190-210 g, Vogel conflict drinking test model)[2]
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Dosage:0.03 mg/kg; 0.1 mg/kg; 0.3 mg/kg
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Administration:p.o.; single dose; 1 hour pre-test
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Result:Increased punished drinking time by +165% at 0.03 mg/kg, with further increases at higher doses, reaching significance at all tested doses compared to vehicle.
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Animal Model:NMRI mice (male, ~22 g, stress-induced hyperthermia model)[2]
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Dosage:1 mg/kg; 10 mg/kg; 30 mg/kg
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Administration:p.o.; single dose; 1 hour pre-test
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Result:Reduced stress-induced hyperthermia by -48% at 0.01 mg/kg, -73% at 0.1 mg/kg, and -145% at 1 mg/kg compared to vehicle, with all doses producing significant effects.
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Animal Model:Sprague Dawley rats (male, 350 g, conditioned emotional response model)[2]
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Dosage:0.03 mg/kg; 0.1 mg/kg
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Administration:p.o.; single dose; 1 hour pre-test
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Result:Increased the suppression ratio by +567% at 0.3 mg/kg and +583% at 1 mg/kg compared to vehicle, indicating reduced fear response.
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Animal Model:Sprague Dawley rats (male, 225-287 g, fear-potentiated startle model)[2]
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Dosage:0.03 mg/kg; 0.1 mg/kg
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Administration:p.o.; single dose; 1 hour pre-test
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Result:Reduced fear-potentiated startle amplitude by -53% at 0.1 mg/kg and -94% at 1 mg/kg compared to vehicle, with significant effects at both doses.
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Animal Model:NMRI mice (male, 24-30 g, formalin-induced paw licking model, late phase)[2]
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Dosage:1 mg/kg; 10 mg/kg
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Administration:p.o.; single dose; 40 minutes pre-formalin injection
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Result:Reduced paw licking time by -91% (non-significant) at 1 mg/kg and -95% (significant) at 10 mg/kg compared to vehicle in the late phase of formalin-induced pain.
Had no significant effect in the early phase at any tested dose.
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Animal Model:Sprague Dawley rats (female, 100-250 g, Bennett model of cold allodynia with sciatic nerve constriction injury)[2]
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Dosage:0.1 mg/kg; 0.3 mg/kg; 1 mg/kg; 3 mg/kg; 10 mg/kg
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Administration:s.c.; single dose; 60 minutes pre-test
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Result:Increased the inhibition rate of cold allodynia by 28% at 0.1 mg/kg, 37% at 0.3 mg/kg, 50% at 1 mg/kg, 39% at 3 mg/kg, and 58% at 10 mg/kg compared to vehicle.
Produced significant effects at all doses, with maximal efficacy comparable to morphine (64% inhibition rate) and duloxetine (56% inhibition rate).
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Animal Model:Sprague Dawley rats (female, 200-250 g, volume-induced micturition reflex model with cannulated bladders, anesthetized)[2]
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Dosage:0.03 mg/kg; 0.3 mg/kg
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Administration:i.v.; single dose
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Result:Increased the micturition threshold volume by +27% at 0.03 mg/kg and +166.9% at 0.3 mg/kg compared to baseline, with significant effects at both doses.
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Animal Model:Sprague Dawley rats (female, 200-250 g, isovolumetric bladder contraction model with cannulated bladders, anesthetized)[2]
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Dosage:0.01 mg/kg; 0.03 mg/kg
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Administration:i.v.; single dose
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Result:Reduced bladder contraction frequency by -88.5% at 0.01 mg/kg and -79.9% at 0.03 mg/kg compared to vehicle, with maximal effects comparable at both doses.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 802906-73-6
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Appearance Solid
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분자량 325.77
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화학식 C18H13ClFN3
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Color Off-white to yellow
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SMILES
CC1=C(C#CC2=CC(Cl)=NC=C2)N=C(C)N1C3=CC=C(F)C=C3
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Synonyms
RG7090; RO4917523
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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 (1)
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Journal Impact Factor
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Most Recent
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ACS Chem Neurosci
Location and Cell-Type-Specific Bias of Metabotropic Glutamate Receptor, mGlu5, Negative Allosteric Modulators. [Abstract]2019 Nov 20;10(11):4558-4570. PMID: 31609579
용액&용해도
DMSO : ≥ 33.33 mg/mL (102.31 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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: ≥ 2.5 mg/mL (7.67 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 (7.67 mM); Suspended solution; Need ultrasonic and warming
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.
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 (297 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Jaeschke G, et al. Metabotropic glutamate receptor 5 negative allosteric modulators: discovery of 2-chloro-4-[1-(4-fluorophenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]pyridine (basimglurant, RO4917523), a promising novel medicine for psychiatric diseases. [Content Brief]
[2]. Lindemann L, et al. Pharmacology of basimglurant (RO4917523, RG7090), a unique metabotropic glutamate receptor 5 negative allosteric modulator in clinical development for depression. J Pharmacol Exp Ther. 2015 Apr;353(1):213-33. [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, 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 | 3.0697 mL | 15.3483 mL | 30.6965 mL | 76.7413 mL |
| 5 mM | 0.6139 mL | 3.0697 mL | 6.1393 mL | 15.3483 mL | |
| 10 mM | 0.3070 mL | 1.5348 mL | 3.0697 mL | 7.6741 mL | |
| 15 mM | 0.2046 mL | 1.0232 mL | 2.0464 mL | 5.1161 mL | |
| 20 mM | 0.1535 mL | 0.7674 mL | 1.5348 mL | 3.8371 mL | |
| 25 mM | 0.1228 mL | 0.6139 mL | 1.2279 mL | 3.0697 mL | |
| 30 mM | 0.1023 mL | 0.5116 mL | 1.0232 mL | 2.5580 mL | |
| 40 mM | 0.0767 mL | 0.3837 mL | 0.7674 mL | 1.9185 mL | |
| 50 mM | 0.0614 mL | 0.3070 mL | 0.6139 mL | 1.5348 mL | |
| 60 mM | 0.0512 mL | 0.2558 mL | 0.5116 mL | 1.2790 mL | |
| 80 mM | 0.0384 mL | 0.1919 mL | 0.3837 mL | 0.9593 mL | |
| 100 mM | 0.0307 mL | 0.1535 mL | 0.3070 mL | 0.7674 mL |
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