Sumatriptan Succinate (GR43175)

Alias: GR 43175; Sumatriptan; GR-43175; GR43175;Sumatran; Sumax
Cat No.:V0988 Purity: = 99.52%
Sumatriptan Succinate (GR-43175; GR43175; Sumatran; Sumax), an approved triptan sulfa drug and a sulfonamide compound, is a selective 5-HT1 receptor agonist used for the treatment of migraine headaches.
Sumatriptan Succinate (GR43175) Chemical Structure CAS No.: 103628-48-4
Product category: 5-HT Receptor
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
10mg
100mg
250mg
500mg
1g
2g
Other Sizes

Other Forms of Sumatriptan Succinate (GR43175):

  • Sumatriptan
  • Sumatriptan HCl
Official Supplier of:
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Top Publications Citing lnvivochem Products
Purity & Quality Control Documentation

Purity: = 99.52%

Product Description

Sumatriptan Succinate (GR-43175; GR43175; Sumatran; Sumax), an approved triptan sulfa drug and a sulfonamide compound, is a selective 5-HT1 receptor agonist used for the treatment of migraine headaches. It is selective to 5-HT1A, 5-HT1B, and 5-HT1D. Its succinate salt is called sumatriptan succinate.

Biological Activity I Assay Protocols (From Reference)
Targets
5-HT1D Receptor ( Ki = 17 nM ); 5-HT1B Receptor ( Ki = 27 nM ); 5-HT1A Receptor ( IC50 = 100 nM )
ln Vitro

In vitro activity: Sumatriptan is slightly less effective at 5-HT1A binding sites (Ki = 100 nM) but exhibits the highest affinity for 5-HT1D (Ki = 17 nM) and 5-HT1B (Ki = 27 nM) binding sites. The effects of electrical stimulation of the trigeminal ganglion on plasma protein extravasation are significantly reduced by sumatriptan. The morphological alterations in mast cells and post-capillary venules within the dura mater that occur after electrical trigeminal ganglion stimulation are lessened by sumatriptan.

ln Vivo
In rats with a trigeminal neuropathic pain model, sumatriptan at a clinically relevant dose (100 mg/kg, s.c.) significantly reduces the mechanical allodynia-like behavior on both the injured and contralateral sides (peak-effects 6.3 g and 4.4 g, respectively). Following mechanical stimulation in cats, sumatriptan decreases the number of Fos-positive cells (6, 13 cells and 9 cells, respectively) in laminae I and IIo of the trigeminal nucleus caudalis and C2. Sumatriptan selectively constricts the cranial vessels that are enlarged and inflamed during a migraine attack; this action is mediated by activating a subtype of 5-HT1 receptor that has been localized in cranial vessels in animals. Oral bioavailabilities of sumatriptan in rats, dogs, and rabbits are 37, 58, and 23%, respectively. In rats, dogs, and rabbits, sumatriptan has a half-life of 1-2 hours and is rapidly eliminated by metabolic and renal processes. Although it is less well tolerated in dogs, sumatriptan has few negative pharmacodynamic effects when given acutely, with the exception of high doses.
Animal Protocol


References

[1]. Eur J Pharmacol . 1989 Apr 12;163(1):133-6.

[2]. Br J Pharmacol . 2002 Dec;137(8):1287-97.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C18H27N3O6S
Molecular Weight
413.49
Exact Mass
413.16
Elemental Analysis
C, 52.29; H, 6.58; N, 10.16; O, 23.22; S, 7.75
CAS #
103628-48-4
Related CAS #
Sumatriptan; 103628-46-2; Sumatriptan hydrochloride; 103628-62-2; 143675-45-0 (hemisulfate)
Appearance
White to off-white solid powder
SMILES
CNS(=O)(=O)CC1=CC2=C(C=C1)NC=C2CCN(C)C.C(CC(=O)O)C(=O)O
InChi Key
PORMUFZNYQJOEI-UHFFFAOYSA-N
InChi Code
InChI=1S/C14H21N3O2S.C4H6O4/c1-15-20(18,19)10-11-4-5-14-13(8-11)12(9-16-14)6-7-17(2)3;5-3(6)1-2-4(7)8/h4-5,8-9,15-16H,6-7,10H2,1-3H3;1-2H2,(H,5,6)(H,7,8)
Chemical Name
butanedioic acid;1-[3-[2-(dimethylamino)ethyl]-1H-indol-5-yl]-N-methylmethanesulfonamide
Synonyms
GR 43175; Sumatriptan; GR-43175; GR43175;Sumatran; Sumax
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 50~83 mg/mL (120.9~200.7 mM)
Water: <1 mg/mL
Ethanol: ~83 mg/mL (~200.7 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.05 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.5 mg/mL (6.05 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

View More

Solubility in Formulation 3: ≥ 2.5 mg/mL (6.05 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.


Solubility in Formulation 4: 100 mg/mL (241.84 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.4184 mL 12.0922 mL 24.1844 mL
5 mM 0.4837 mL 2.4184 mL 4.8369 mL
10 mM 0.2418 mL 1.2092 mL 2.4184 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

  • Calculate the Mass of a compound required to prepare a solution of known volume and concentration
  • Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume
An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
  • To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
/

Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

  • Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
  • Click the “Calculate” button
  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
+
+
+

Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Clinical Trial Information
NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT00356603 Completed Drug: Sumatriptan Succinate Migraine Disorders GlaxoSmithKline June 20, 2006 Phase 3
NCT01269281 Completed Drug: Sumatriptan Healthy Dr. Reddy's Laboratories
Limited
July 2005 Phase 1
NCT01507610 Completed Drug: Sumatriptan Migraine Optinose US Inc. January 2012 Phase 1
NCT00847405 Completed Drug: Sumatriptan Succinate
Drug: Imitrex®
Healthy Teva Pharmaceuticals USA March 2003 Phase 1
NCT00846885 Recruiting Drug: Sumatriptan Succinate
Drug: Imitrex®
Healthy Teva Pharmaceuticals USA August 2004 Phase 1
Biological Data
  • Sumatriptan Succinate
    Time-course curves of the effects of various doses of sumatriptan or saline on the mechanical response thresholds in the infraorbital nerve territory ipsilateral and contralateral to the ligature.Br J Pharmacol.2002 Dec;137(8):1287-97.
  • Sumatriptan Succinate
    Br J Pharmacol.2002 Dec;137(8):1287-97.
Contact Us Back to top