Brimonidine Tartrate
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MedKoo CAT#: 317332

CAS#: 70359-46-5 (tartrate)

Description: Brimonidine tartrate is a selective AR, α 2 receptor, agonist used to treat glaucoma. Upon ocular administration, brimonidine tartrate acts on the blood vessels causing them to constrict which leads to a decrease in the production of aqueous humor. Brimonidine tartrate enhances the outflow of aqueous humor. This drug is used to reduce intraocular pressure.

Chemical Structure

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Brimonidine Tartrate
CAS# 70359-46-5 (tartrate)
Instruction

Theoretical Analysis

MedKoo Cat#: 317332
Name: Brimonidine Tartrate
CAS#: 70359-46-5 (tartrate)
Chemical Formula: C15H16BrN5O6
Exact Mass: 0.00
Molecular Weight: 442.220
Elemental Analysis: C, 40.74; H, 3.65; Br, 18.07; N, 15.84; O, 21.71

Price and Availability

Size Price Availability Quantity
10mg USD 160
25mg USD 190
50mg USD 280
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Related CAS #: 59803-98-4 (free base)   70359-46-5 (tartrate)    

Synonym: Brimonidine Tartrate; AGN 190342; AGN-190342; AGN190342; Alphagan; UK 14,304-18; UK 14,304; UK 14304; UK-14,304-18; UK-14,308

IUPAC/Chemical Name: 5-bromo-N-(4,5-dihydro-1H-imidazol-2-yl)quinoxalin-6-amine;(2R,3R)-2,3-dihydroxybutanedioic acid

InChi Key: QZHBYNSSDLTCRG-UHFFFAOYSA-N

InChi Code: InChI=1S/C11H10BrN5.C4H6O6/c12-9-7(17-11-15-5-6-16-11)1-2-8-10(9)14-4-3-13-8;5-1(3(7)8)2(6)4(9)10/h1-4H,5-6H2,(H2,15,16,17);1-2,5-6H,(H,7,8)(H,9,10)

SMILES Code: C1CN=C(N1)NC2=C(C3=NC=CN=C3C=C2)Br.C(C(C(=O)O)O)(C(=O)O)O

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 442.22 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Jackson JM, Knuckles M, Minni JP, Johnson SM, Belasco KT. The role of
brimonidine tartrate gel in the treatment of rosacea. Clin Cosmet Investig
Dermatol. 2015 Oct 23;8:529-38. doi: 10.2147/CCID.S58920. eCollection 2015.
Review. PubMed PMID: 26566370; PubMed Central PMCID: PMC4627400.


2: Erratum: The efficacy and safety of add-on 0.1% brimonidine tartrate preserved
with sodium chlorite in on-treatment Japanese normal-tension glaucoma patients
[Corrigendum]. Clin Ophthalmol. 2015 Jul 22;9:1365. doi: 10.2147/OPTH.S91388.
eCollection 2015. PubMed PMID: 26229429; PubMed Central PMCID: PMC4516178.


3: Johnson AW, Johnson SM. The Role of Topical Brimonidine Tartrate Gel as a
Novel Therapeutic Option for Persistent Facial Erythema Associated with Rosacea.
Dermatol Ther (Heidelb). 2015 Sep;5(3):171-81. doi: 10.1007/s13555-015-0078-1.
Epub 2015 Jun 26. PubMed PMID: 26112098; PubMed Central PMCID: PMC4580655.


4: Takamura Y, Tomomatsu T, Matsumura T, Takihara Y, Kozai S, Arimura S, Yokota
S, Inatani M. Vitreous and aqueous concentrations of brimonidine following
topical application of brimonidine tartrate 0.1% ophthalmic solution in humans. J
Ocul Pharmacol Ther. 2015 Jun;31(5):282-5. doi: 10.1089/jop.2015.0003. Epub 2015
Apr 28. PubMed PMID: 25918904.


5: Erratum: The efficacy and safety of add-on 0.1% brimonidine tartrate preserved
with sodium chlorite in on-treatment Japanese normal-tension glaucoma patients
[Corrigendum]. Clin Ophthalmol. 2015 Mar 9;9:453. doi: 10.2147/OPTH.S81448.
eCollection 2015. PubMed PMID: 25834381; PubMed Central PMCID: PMC4358649.


6: Del Rosso JQ. Reply to "Allergic contact dermatitis to topical brimonidine
tartrate gel 0.33% for treatment of rosacea". J Am Acad Dermatol. 2014
Oct;71(4):833-4. doi: 10.1016/j.jaad.2014.06.040. PubMed PMID: 25219709.


7: Swanson LA, Warshaw EM. Allergic contact dermatitis to topical brimonidine
tartrate gel 0.33% for treatment of rosacea. J Am Acad Dermatol. 2014
Oct;71(4):832-3. doi: 10.1016/j.jaad.2014.05.073. PubMed PMID: 25219708.


8: Tsumura T, Yoshikawa K, Kimura T, Suzumura H, Kawashima M, Nanno M, Ishijima
K, Takeda R. The efficacy and safety of add-on 0.1% brimonidine tartrate
preserved with sodium chlorite in on-treatment Japanese normal-tension glaucoma
patients. Clin Ophthalmol. 2014 Sep 1;8:1681-7. doi: 10.2147/OPTH.S67366.
eCollection 2014. Erratum in: Clin Ophthalmol. 2015;9:453. Clin Ophthalmol.
2015;9:1365. PubMed PMID: 25214761; PubMed Central PMCID: PMC4159391.


9: Dubey A, Prabhu P. Formulation and evaluation of stimuli-sensitive hydrogels
of timolol maleate and brimonidine tartrate for the treatment of glaucoma. Int J
Pharm Investig. 2014 Jul;4(3):112-8. doi: 10.4103/2230-973X.138340. PubMed PMID:
25126524; PubMed Central PMCID: PMC4131382.


10: Tong LX, Moore AY. Brimonidine tartrate for the treatment of facial flushing
and erythema in rosacea. Expert Rev Clin Pharmacol. 2014 Sep;7(5):567-77. doi:
10.1586/17512433.2014.945910. Epub 2014 Aug 4. Review. PubMed PMID: 25091290.


11: Fowler J, Tan J, Jackson JM, Meadows K, Jones T, Jarratt M, Leoni M;
Brimonidine Phase III Study Group. Treatment of facial erythema in patients with
rosacea with topical brimonidine tartrate: correlation of patient satisfaction
with standard clinical endpoints of improvement of facial erythema. J Eur Acad
Dermatol Venereol. 2015 Mar;29(3):474-81. doi: 10.1111/jdv.12587. Epub 2014 Jul
30. PubMed PMID: 25074756.


12: Ibrahim F, El-Enany N, El-Shaheny RN, Mikhail IE. Validated
spectrofluorimetric and spectrophotometric methods for the determination of
brimonidine tartrate in ophthalmic solutions via derivatization with NBD-Cl.
Application to stability study. Luminescence. 2015 May;30(3):309-17. doi:
10.1002/bio.2730. Epub 2014 Jul 10. PubMed PMID: 25044105.


13: Fedorchak MV, Conner IP, Medina CA, Wingard JB, Schuman JS, Little SR. 28-day
intraocular pressure reduction with a single dose of brimonidine tartrate-loaded
microspheres. Exp Eye Res. 2014 Aug;125:210-6. doi: 10.1016/j.exer.2014.06.013.
Epub 2014 Jun 28. PubMed PMID: 24983144.


14: Jackson JM, Fowler J, Moore A, Jarratt M, Jones T, Meadows K, Steinhoff M,
Rudisill D, Leoni M; Brimonidine Phase III Study Group. Improvement in facial
erythema within 30 minutes of initial application of brimonidine tartrate in
patients with rosacea. J Drugs Dermatol. 2014 Jun;13(6):699-704. PubMed PMID:
24918560.


15: Abramovits W, Prato A, Vincent KD, Scheinfeld N, Gupta AK. MIRVASO
(brimonidine tartrate) topical gel 0.33%. Skinmed. 2014 Jan-Feb;12(1):41-3.
PubMed PMID: 24720083.


16: Sunitha G, Bhagirath R, Alapati VR, Ramakrishna K, Subrahmanyam CV, Anumolu
PD. Fluorimetric quantification of brimonidine tartrate in eye drops. Indian J
Pharm Sci. 2013 Nov;75(6):730-2. PubMed PMID: 24591750; PubMed Central PMCID:
PMC3928739.


17: Benkali K, Leoni M, Rony F, Bouer R, Fernando A, Graeber M, Wagner N.
Comparative pharmacokinetics and bioavailability of brimonidine following ocular
and dermal administration of brimonidine tartrate ophthalmic solution and gel in
patients with moderate-to-severe facial erythema associated with rosacea. Br J
Dermatol. 2014 Jul;171(1):162-9. doi: 10.1111/bjd.12881. Epub 2014 Jul 16. PubMed
PMID: 24506775.


18: Routt ET, Levitt JO. Rebound erythema and burning sensation from a new
topical brimonidine tartrate gel 0.33%. J Am Acad Dermatol. 2014 Feb;70(2):e37-8.
doi: 10.1016/j.jaad.2013.10.054. PubMed PMID: 24438976.


19: Moore A, Kempers S, Murakawa G, Weiss J, Tauscher A, Swinyer L, Liu H, Leoni
M. Long-term safety and efficacy of once-daily topical brimonidine tartrate gel
0.5% for the treatment of moderate to severe facial erythema of rosacea: results
of a 1-year open-label study. J Drugs Dermatol. 2014 Jan;13(1):56-61. PubMed
PMID: 24385120.


20: Ravindran VK, Repala S, Subadhra S, Appapurapu AK. Chick chorioallantoic
membrane model for in ovo evaluation of timolol maleate-brimonidine tartrate
ocular inserts. Drug Deliv. 2014 Jun;21(4):307-14. doi:
10.3109/10717544.2013.845272. Epub 2013 Oct 17. PubMed PMID: 24134746.