Lodoxamide Tromethamide | CAS#63610-09-3

MedKoo Cat#: 526636 | Name: Lodoxamide Tromethamide

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Lodoxamide Tromethamide is a mast-cell stabilizer, inhibiting type I immediate hypersensitivity reaction by preventing the antigen-stimulated calcium influx into mast cells and the release of slow-reacting substances of anaphylaxis (SRS-A).

Chemical Structure

Lodoxamide Tromethamide

CAS#63610-09-3 (Tromethamide)

Theoretical Analysis

MedKoo Cat#: 526636

Name: Lodoxamide Tromethamide

CAS#: 63610-09-3 (Tromethamide)

Chemical Formula: C19H28ClN5O12

Exact Mass: 0.0000

Molecular Weight: 553.91

Elemental Analysis: C, 41.20; H, 5.10; Cl, 6.40; N, 12.64; O, 34.66

Price and Availability

Size	Price	Availability
50mg	USD 250.00	2 Weeks
100mg	USD 400.00	2 weeks
250mg	USD 750.00	2 weeks
1g	USD 1,250.00	2 weeks

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Related CAS #

63610-09-3 (Tromethamide) 53882-12-5

Synonym

Lodoxamide Tromethamide; Alomide

IUPAC/Chemical Name

{3-[(carboxycarbonyl)amino]-2-chloro-5-cyanoanilino}(oxo)acetic acid compound with 2-amino-2-(hydroxymethyl)-1,3-propanediol (1:2)

InChi Key

JJOFNSLZHKIJEV-UHFFFAOYSA-N

InChi Code

InChI=1S/C11H6ClN3O6.2C4H11NO3/c12-7-5(14-8(16)10(18)19)1-4(3-13)2-6(7)15-9(17)11(20)21;2*5-4(1-6,2-7)3-8/h1-2H,(H,14,16)(H,15,17)(H,18,19)(H,20,21);2*6-8H,1-3,5H2

SMILES Code

O=C(O)C(NC1=CC(C#N)=CC(NC(C(O)=O)=O)=C1Cl)=O.OCC(CO)(N)CO.OCC(CO)(N)CO

Appearance

Solid powder

Purity

>95% (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

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

Product Data

Product Data

Instruction

View handling instruction

Biological target:

Lodoxamide tromethamine (U-42585E) is a medication for the treatment of prophylaxis of mast cell-mediated allergic disease.

In vitro activity:

Lodoxamide was also able to strongly inhibit the release of eosinophil peroxidase after IgA-dependent activation and, to a lesser extent, the release of eosinophil cationic protein and eosinophil-derived neurotoxin. Taken together, these results indicate that lodoxamide can exert potent inhibitory effects on eosinophil activation in vitro combined with a strong inhibition of eosinophil attraction, leading therefore to a reduction in their pathological potential in vivo. Reference: Int Arch Allergy Immunol. 1998 Jun;116(2):140-6. https://pubmed.ncbi.nlm.nih.gov/9652307/

In vivo activity:

This study hypothesized that adding an inhibitor of mast cell degranulation, lodoxamide tromethamine (10 micromol/L), to Euro-Collins and University of Wisconsin preservation solutions, would decrease lung preservation injury in rat lungs. After 12 hours of ischemic storage, lodoxamide tromethamine-enhanced Euro-Collins solution decreased alveolar-arterial oxygen difference from 588 to 485 (p < 0.001), increased oxygen tension from 100 to 161 mm Hg (p = 0.012), decreased capillary filtration coefficient from 6.2 to 2.6 (p < 0.001), and increased compliance from 0.12 to 0.21 (p < 0.001); lodoxamide tromethamine-enhanced University of Wisconsin solution decreased alveolar-arterial oxygen difference from 478 to 322 (p < 0.001), increased oxygen tension from 214 to 335 mm Hg (p < 0.001), decreased capillary filtration constant from 4.2 to 2.0 (p < 0.001), and increased compliance from 0.20 to 0.25 (p < 0.001). Reference: J Thorac Cardiovasc Surg. 1998 Mar;115(3):631-6; discussion 636-7. https://pubmed.ncbi.nlm.nih.gov/9535451/

	Solvent	mg/mL	mM
Solubility
	DMSO	20.0	46.21
	Water	59.5	137.49

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 553.91 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.

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:

1. Capron M, Loiseau S, Papin JP, Robertson S, Capron A. Inhibitory effects of lodoxamide on eosinophil activation. Int Arch Allergy Immunol. 1998 Jun;116(2):140-6. doi: 10.1159/000023937. PMID: 9652307. 2. Kim MJ, Park SJ, Nam SY, Im DS. Lodoxamide Attenuates Hepatic Fibrosis in Mice: Involvement of GPR35. Biomol Ther (Seoul). 2019 Jun 13;28(1):92-97. doi: 10.4062/biomolther.2018.227. Epub ahead of print. PMID: 31189299; PMCID: PMC6939691. 3. Barr ML, Carey JN, Nishanian GP, Roberts RF, Sakamaki Y, Darbinian SH, Starnes VA. Addition of a mast cell stabilizing compound to organ preservation solutions decreases lung reperfusion injury. J Thorac Cardiovasc Surg. 1998 Mar;115(3):631-6; discussion 636-7. doi: 10.1016/S0022-5223(98)70328-9. PMID: 9535451.

In vitro protocol:

In vivo protocol:

1. Kim MJ, Park SJ, Nam SY, Im DS. Lodoxamide Attenuates Hepatic Fibrosis in Mice: Involvement of GPR35. Biomol Ther (Seoul). 2019 Jun 13;28(1):92-97. doi: 10.4062/biomolther.2018.227. Epub ahead of print. PMID: 31189299; PMCID: PMC6939691. 2. Barr ML, Carey JN, Nishanian GP, Roberts RF, Sakamaki Y, Darbinian SH, Starnes VA. Addition of a mast cell stabilizing compound to organ preservation solutions decreases lung reperfusion injury. J Thorac Cardiovasc Surg. 1998 Mar;115(3):631-6; discussion 636-7. doi: 10.1016/S0022-5223(98)70328-9. PMID: 9535451.

1: Zhang W, Lin Z. Contrast of the effect of alomide and sodium cromoglycate in the treatment of allergic eye diseases. Yan Ke Xue Bao. 2000 Sep;16(3):214-6. PubMed PMID: 12579651. 2: Oguz H, Bitiren M, Aslan OS, Ozardali I. Efficacy of lodoxamide eye drops on tear fluid cytology of patients with vernal conjunctivitis. Acta Med Okayama. 1999 Jun;53(3):123-6. PubMed PMID: 10410789. 3: Denis D, Bloch-Michel E, Verin P, Sebastiani A, Tazartes M, Helleboid L, Di Giovanni A, Lecorvec M. Treatment of common ocular allergic disorders; a comparison of lodoxamide and NAAGA. Br J Ophthalmol. 1998 Oct;82(10):1135-8. PubMed PMID: 9924299; PubMed Central PMCID: PMC1722390. 4: Kabat AG. Lacrimal occlusion therapy for the treatment of superior limbic keratoconjunctivitis. Optom Vis Sci. 1998 Oct;75(10):714-8. PubMed PMID: 9798210. 5: Maĭchuk IuF, Khaitova KN, Grishakova MB. [Alomide eyedrops in the treatment of allergic conjunctivitis and keratoconjunctivitis]. Vestn Oftalmol. 1998 Jul-Aug;114(4):43-4. Russian. PubMed PMID: 9771090. 6: Barr ML, Carey JN, Nishanian GP, Roberts RF, Sakamaki Y, Darbinian SH, Starnes VA. Addition of a mast cell stabilizing compound to organ preservation solutions decreases lung reperfusion injury. J Thorac Cardiovasc Surg. 1998 Mar;115(3):631-6; discussion 636-7. PubMed PMID: 9535451. 7: Humphreys RA, Kane KA, Parratt JR. Lack of involvement of mast cell degranulation in the antiarrhythmic effect of preconditioning in rats. J Cardiovasc Pharmacol. 1998 Mar;31(3):418-23. PubMed PMID: 9514187. 8: Krásný J. [Alomide, a preventive immunopharmaceutical agent, in the treatment of ocular atopy]. Cesk Slov Oftalmol. 1998 Jan;54(1):41-5. Czech. PubMed PMID: 9501643. 9: Bonini S, Schiavone M, Bonini S, Magrini L, Lischetti P, Lambiase A, Bucci MG. Efficacy of lodoxamide eye drops on mast cells and eosinophils after allergen challenge in allergic conjunctivitis. Ophthalmology. 1997 May;104(5):849-53. PubMed PMID: 9160033. 10: Ciprandi G, Buscaglia S, Catrullo A, Paolieri F, Riccio AM, Fiorino N, Canonica GW. Antiallergic activity of topical lodoxamide on in vivo and in vitro models. Allergy. 1996 Dec;51(12):946-51. PubMed PMID: 9020426. 11: Friedlaender MH. Contact lens induced conjunctivitis: a model of human ocular inflammation. CLAO J. 1996 Jul;22(3):205-8. PubMed PMID: 8828938. 12: van Haaster CM, Engels W, Duijvestijn AM, Lemmens PJ, Hornstra G, Van der Vusse GJ. Lack of evidence for a role of mast cell degranulation in acute hypoxia/reoxygenation-induced injury in the isolated rat heart. J Mol Cell Cardiol. 1996 Feb;28(2):363-73. PubMed PMID: 8729068. 13: Grutzmacher RD, Foster RS, Feiler LS. Lodoxamide tromethamine treatment for superior limbic keratoconjunctivitis. Am J Ophthalmol. 1995 Sep;120(3):400-2. PubMed PMID: 7661218. 14: Cerqueti PM, Ricca V, Tosca MA, Buscaglia S, Ciprandi G. Lodoxamide treatment of allergic conjunctivitis. Int Arch Allergy Immunol. 1994 Oct;105(2):185-9. PubMed PMID: 7920019. 15: Hussar DA. New therapeutic agents marketed in 1993. Pa Med. 1994 Jul;97(7):16-8. PubMed PMID: 7936695. 16: Parenteau GL, Clark RE. Prevention of ischemia-reperfusion injury by the allergy drug lodoxamide tromethamine. Ann Thorac Surg. 1991 Oct;52(4):832-8. PubMed PMID: 1929638. 17: Veal CF Jr, Jackson RM, Brannen AL, Fulmer JD. Lodoxamide tromethamine prevents neutrophil accumulation in reexpansion pulmonary edema. J Cardiovasc Pharmacol. 1989 Aug;14(2):227-32. PubMed PMID: 2476595. 18: Till GO, Guilds LS, Mahrougui M, Friedl HP, Trentz O, Ward PA. Role of xanthine oxidase in thermal injury of skin. Am J Pathol. 1989 Jul;135(1):195-202. PubMed PMID: 2549794; PubMed Central PMCID: PMC1880226. 19: Schmeling DJ, Drongowski RA, Coran AG. The beneficial effects of ibuprofen on a lethal live E. coli septic shock model and the relationship of these effects to superoxide radical production. Prog Clin Biol Res. 1989;299:53-61. PubMed PMID: 2542991. 20: Keller AM, Clancy RM, Barr ML, Marboe CC, Cannon PJ. Acute reoxygenation injury in the isolated rat heart: role of resident cardiac mast cells. Circ Res. 1988 Dec;63(6):1044-52. PubMed PMID: 2848639.