Atreleuton - CAS 154355-76-7
Catalog number: 154355-76-7
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C16H15FN2O2S
Molecular Weight:
318.37
COA:
Inquire
Targets:
Leukotriene Receptor | Lipoxygenases (LOXs)
Description:
Atreleuton, a kind of urea compound, has been found to be a 5-lipoxygenase inhibitor as well as Leukotriene B4 receptor antagonist that could probably be useful in study of sorts of diseases like asthma and acute coronary syndromes. It has already been discontinued by VIA Pharmaceuticals.
Purity:
98%
Appearance:
Powder
Synonyms:
Atreleuton; ABT-761; Atreleuton [USAN]; UNII-U301T88E1M; ABT 761; 1-[(2R)-4-[5-[(4-fluorophenyl)methyl]thiophen-2-yl]but-3-yn-2-yl]-1-hydroxyurea
Storage:
Store in a cool and dry place and at 0 - 4 °C for short term (days to weeks) or -20 °C for long term (months to years).
MSDS:
Inquire
Quality Standard:
In-house standard
Quantity:
Milligram-Grams
InChIKey:
MMSNEKOTSJRTRI-LLVKDONJSA-N
InChI:
InChI=1S/C16H15FN2O2S/c1-11(19(21)16(18)20)2-7-14-8-9-15(22-14)10-12-3-5-13(17)6-4-12/h3-6,8-9,11,21H,10H2,1H3,(H2,18,20)/t11-/m1/s1
Canonical SMILES:
CC(C#CC1=CC=C(S1)CC2=CC=C(C=C2)F)N(C(=O)N)O
1.N-hydroxyurea and hydroxamic acid inhibitors of cyclooxygenase and 5-lipoxygenase.
Connolly PJ;Wetter SK;Beers KN;Hamel SC;Chen RH;Wachter MP;Ansell J;Singer MM;Steber M;Ritchie DM;Argentieri DC Bioorg Med Chem Lett. 1999 Apr 5;9(7):979-84.
Two series of compounds (1 and 2) having structural features of the dual COX/5-LO inhibitor tepoxalin and the 5-LO inhibitor ABT-761 were prepared. Many of these hybrid compounds are potent COX and 5-LO inhibitors; two compounds (1a and 2t) inhibit eicosanoid biosynthesis in an ex vivo assay.
2.Pharmacokinetics of a novel 5-lipoxygenase inhibitor (ABT-761) in pediatric patients with asthma.
Wong SL;Kearns GL;Kemp JP;Drajesk J;Chang M;Locke CS;Dube LM;Awni WM Eur J Clin Pharmacol. 1998 Nov-Dec;54(9-10):715-9.
OBJECTIVE: ;The pharmacokinetics of an N-hydroxyurea analog, ABT-761 in asthmatic pediatric patients with asthma were investigated.;METHODS: ;A total of 24 patients were enrolled into this 8-day single- and multiple-dose study. Patients received daily doses of ABT-761 according to their body weight: patients of 20-38 kg received 50 mg; patients >38 kg but < or = 55 kg received 100 mg, and patients >55 kg received 150 mg.;RESULTS: ;The mean values for the terminal phase t1/2 were 16-17 h after multiple-dose administration. When normalized for body weight, the mean day 8 Cl(f) values for 50-, 100-mg, and 150-mg doses were 0.57 (n=13), 0.51 (n=10), and 0.43 (n=1) ml x min(-1) x kg(-1), respectively, while the mean Vz/f values ranged from 0.75 to 0.77 l x kg(-1). The mean accumulation ratio observed (day 8 to day 1 AUC0-24 ratio) of ABT-761 was approximately 1.7, which is consistent with the t1/2 of this drug. Body weight, age, and body surface area were virtually identical in explaining the variability in dose-normalized Cmax and AUC values (R2=0.61-0.68). The percents of variance explained by these three variables were within a range of 3% for each pharmacokinetic parameter.;CONCLUSIONS: ;The pharmacokinetics of ABT-761 in children were similar to those previously reported in adults.
3.Effects of a 5-lipoxygenase inhibitor, ABT-761, on exercise-induced bronchoconstriction and urinary LTE4 in asthmatic patients.
Lehnigk B;Rabe KF;Dent G;Herst RS;Carpentier PJ;Magnussen H Eur Respir J. 1998 Mar;11(3):617-23.
The novel 5-lipoxygenase (5-LO) inhibitor, ABT-761, was investigated for its effect on exercise-induced bronchoconstriction in asthmatic subjects. The relationship between 5-LO inhibition and effects on the response of the airways to exercise was examined. In a double-blind, randomized, crossover clinical trial, 10 patients with mild to moderate persistent asthma (who exhibited a fall in forced expiratory volume in one second (FEV1) > or = 20% following standardized exercise challenge) received 200 mg ABT-761 or matched placebo, orally, 5 h prior to exercise on two study days, 7-10 days apart. Lung function, urinary leukotriene E4 (LTE4) and ex vivo calcium ionophore-stimulated LTB4 release in whole blood were measured prior to dosing, prior to exercise and at various time points up to 4 h post-exercise. The mean (SD) maximal percentage fall in FEV1 after exercise was 27.1 (12)% on placebo and 19.9 (10)% on ABT-761 days, respectively (p<0.05). Post-exercise fall in FEV1 was significantly attenuated at 5, 10, 15 and 30 min after exercise and the mean area under curve, representing the overall effect of exercise from 0-45 min post-challenge, was also significantly attenuated by ABT-761 (p<0.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related Leukotriene Receptor Products


CAS 847163-28-4 ML 351

ML 351
(CAS: 847163-28-4)

ML 351 is a potent and selective inhibitor of 12/15-lipoxygenase (IC50 value 200 nM against human 12/15-LOX), which catalyzes the oxidation of polyunsaturated f...

CAS 107889-31-6 LY-256548

LY-256548
(CAS: 107889-31-6)

LY-25648 is a leukotriene B4 antagonist.

CAS 1232861-58-3 Gemilukast

Gemilukast
(CAS: 1232861-58-3)

This active molecular is an potent dual Leukotriene CysLT1 and CysLT2 Receptor antagonist originated by Ono Pharmaceutical. IC50 values is 1.7nM against human C...

CAS 134002-60-1 CP-85958

CP-85958
(CAS: 134002-60-1)

This active molecular is a selective LTD4 antagonist. CP-85958 may become a clinical candidates for the treatment of asthma in the future.

CAS 40785-97-5 FPL 55712

FPL 55712
(CAS: 40785-97-5)

FPL 55712 is a leukotriene receptor antagonist that inhibits contraction of guinea pig trachealis induced by leukotrienes C4, D4, E4 and F4.

CAS 153227-04-4 LY-306669

LY-306669
(CAS: 153227-04-4)

LY-306669, a tetrazol derivative, has been found to be a leukotriene B4 receptor antagonist that was once studied its effect in acute lung injury.

CAS 132392-39-3 LY 221068

LY 221068
(CAS: 132392-39-3)

LY 221068 is a Lipoxygenase inhibitor originated by Eli Lilly. It is a potent antioxidant with antiinflammatory properties. But no development was reported for ...

CAS 132465-10-2 2-TEDC

2-TEDC
(CAS: 132465-10-2)

2-TEDC is a potent inhibitor of 5-, 12-, and 15-lipoxygenase (IC50 = 0.09, 0.013 and 0.5 μM, respectively).

CAS 155944-23-3 ZM-230487

ZM-230487
(CAS: 155944-23-3)

ZM-230487, a quinolin derivative, has been found to be a 5-lipoxygenase inhibitor as well as Leukotriene D4 receptor antagonist. It was once studied in anti-inf...

CAS 169626-43-1 WAY-126299A

WAY-126299A
(CAS: 169626-43-1)

WAY-126299A, a benzothiazoly derivative, has been found to be a 5-lipoxygenase inhibitor as well as Leukotriene D4 receptor antagonist and was once studied in A...

CAS 125617-94-9 iralukast

iralukast
(CAS: 125617-94-9)

Iralukast is a Leukotriene D4 receptor antagonist originated by Novartis as a a structural analogue of LTD4. It is applicated for the treatment of asthma and in...

CAS 148291-65-0 LY 210073

LY 210073
(CAS: 148291-65-0)

LY 210073, an oxoxanthene derivative, has been found to be a LTB4 receptor antagonist that could probably be effective against inflammation and rheumatic disord...

CAS 175212-04-1 CMI-977

CMI-977
(CAS: 175212-04-1)

CMI-977, an oxolan compound, has been found to be a 5-Lipoxygenases inhibitor and was once studied as an antiasthmatic agent.

CAS 15722-48-2 Olsalazine

Olsalazine
(CAS: 15722-48-2)

Olsalazine, a kind of colchicum alkaloid, has been found to be an anti-inflammatory agent and could be used against inflammatory bowel disease and ulcerative co...

CAS 122009-61-4 LY 203647

LY 203647
(CAS: 122009-61-4)

LY 203647 is a a leukotriene D4 and E4 receptor antagonist with a tetrazole nucleus structure originated by Eli Lilly. No development for treatment of Ischaemic...

CAS 115103-85-0 MK-571 sodium salt hydrate

MK-571 sodium salt hydrate
(CAS: 115103-85-0)

The sodium salt hydrate of MK-571 which is an effective antagonist of CysLT1 receptor and an inhibitor of MRP1.

CAS 120443-16-5 Verlukast

Verlukast
(CAS: 120443-16-5)

This active molecular is a R-enantiomer of MK-571 which is a selective LTD4 receptor antagonist. Verlukast showed [3H]leukotriene D4 binding in guinea-pig with ...

CAS 169626-43-1 WAY-126299A

WAY-126299A
(CAS: 169626-43-1)

WAY-126299A, a benzothiazoly derivative, has been found to be a 5-lipoxygenase inhibitor as well as Leukotriene D4 receptor antagonist and was once studied in A...

CAS 154355-76-7 Atreleuton

Atreleuton
(CAS: 154355-76-7)

Atreleuton, a kind of urea compound, has been found to be a 5-lipoxygenase inhibitor as well as Leukotriene B4 receptor antagonist that could probably be useful...

CAS 217799-03-6 KP496

KP496
(CAS: 217799-03-6)

KP496, a novel dual antagonist of cysLT receptor and TP, is currently in clinical development as a dry powder inhaler. KP496 inhibited epithelial hypertrophy an...

Chemical Structure

CAS 154355-76-7 Atreleuton

Quick Inquiry

Verification code

Featured Items