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MN-001 Sale

(Synonyms: 4-[6-乙酰基-3-[3-[(4-乙酰基-3-羟基-2-丙基苯基)硫]丙氧基]-2-丙基苯氧基]丁酸,KCA 757, Tipelukast) 目录号 : GC31832

An anti-inflammatory agent

MN-001 Chemical Structure

Cas No.:125961-82-2

规格 价格 库存 购买数量
1 mg
¥630.00
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5 mg
¥2,520.00
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10 mg
¥4,320.00
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产品描述

MN-001 is an anti-inflammatory agent.1 In vivo, MN-001 (10, 30, and 50 mg/kg) reduces the frequency of bladder voids, increases the intercontractile interval, and decreases the number of non-voiding contractions in a rat model of bladder hyperactivity induced by ovalbumin-induced mast cell stimulation.

1.Rajasekaran, M., Locke, K.W., and Parsons, C.L.MN-001, a novel oral anti-inflammatory agent, suppresses bladder hyperactivity in a rat modelBJU Int.98(2)430-434(2006)

Chemical Properties

Cas No. 125961-82-2 SDF
别名 4-[6-乙酰基-3-[3-[(4-乙酰基-3-羟基-2-丙基苯基)硫]丙氧基]-2-丙基苯氧基]丁酸,KCA 757, Tipelukast
化学名 4-[6-acetyl-3-[3-[(4-acetyl-3-hydroxy-2-propylphenyl)thio]propoxy]-2-propylphenoxy]-butanoic acid
Canonical SMILES CC(C1=C(O)C(CCC)=C(SCCCOC2=C(CCC)C(OCCCC(O)=O)=C(C(C)=O)C=C2)C=C1)=O
分子式 C29H38O7S 分子量 530.67
溶解度 1mg/ml in ethanol, sparingly soluable in chloroform & ethyl acetate 储存条件 Store at -20°C
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1 mg 5 mg 10 mg
1 mM 1.8844 mL 9.4221 mL 18.8441 mL
5 mM 0.3769 mL 1.8844 mL 3.7688 mL
10 mM 0.1884 mL 0.9422 mL 1.8844 mL
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Research Update

MN 001: KCA 757, KCA-757, MN-001

MN 001 is an orally bioavailable anti-inflammatory agent, originated by Kyorin Pharmaceutical, which is being developed in clinical trials by the US company MediciNova for the treatment of interstitial cystitis and asthma. Kyorin is developing the drug as KCA 757 for these indications. The actions of the drug are described by MediciNova as consisting of eosinophil migration inhibition, leukotriene antagonism, and phosphodiesterase IV inhibition. Other mechanisms described for MN 001 include the inhibition of phosphodiesterases III, 5-lipoxy-genase, phospholipase C as well as thromboxane A2. Development of an immediate-release formulation of MN 001 has been discontinued. An extended-release formulation remains in development. MediciNova is looking for partnering/outlicensing opportunities for MN 001 in North America and Europe. MediciNova licensed MN 001 from Kyorin Pharmaceutical in March 2002, and now holds exclusive worldwide rights, excluding Japan, China, Taiwan and South Korea, to develop and commercialise the drug. The phase III clinical programme of immediate-release MN 001 was initiated by Medicinova in the US in November 2006. In the first phase III trial, 705 patients with mild to moderate asthma were to be randomised to receive MN 001 (750 mg twice daily, 500 mg three times daily) or placebo for 12 weeks. The change from baseline in mean forced expiratory volume in 1 second (FEV(1)) will be the primary endpoint. The primary endpoint was met in a phase II study of MN 001 in patients with mild to moderate asthma. The trial evaluated the efficacy of three different doses of MN 001 for the treatment of asthma. Results have been reported. MediciNova has received Notices of Allowance from the US Patent and Trademark Office for three patent applications covering certain compositions, uses and manufacturing processes associated with MN 001. MN 001 has received patent protection through at least 2023.

MN-001, a novel oral anti-inflammatory agent, suppresses bladder hyperactivity in a rat model

Objective: To evaluate the effects of MN-001, a novel orally active anti-inflammatory agent, in suppressing the bladder hyperactivity resulting from ovalbumin (OA)-induced mast-cell stimulation in a rat model.
Materials and methods: Sprague-Dawley rats of both sexes were divided into five groups of 10 each, with group 1 as the control and groups 2-5 undergoing OA sensitization to produce mast-cell degranulation using an established method. At 14 days after sensitization, rats were given an acute intravesical challenge: in group 1, by saline (control), and in groups 2-5, with approximately 2 mL of OA (10 mg/mL in sterile saline). Groups 3-5 received the investigational agent MN-001 orally at 10, 30 or 50 mg/kg, respectively, 1 h before intravesical OA challenge. Urodynamics were then evaluated to quantify the frequency of contractions (voids), intercontractile interval (ICI) and non-voiding contractions (NVCs).
Results: Acute intravesical OA challenge in rats in group 2 caused contractions of bladder smooth muscle, leading to a significant (P < 0.05) dose-dependent increase in NVCs and a decrease in ICI. Rats pre-treated with MN-001 at 30 and 50 mg/kg (groups 4 and 5) had significantly fewer NVCs and a greater ICI than rats in group 2 (P < 0.05).
Conclusion: OA challenge in OA-sensitized rats produces bladder hyperactivity, as reflected in significantly more NVCs and a lower ICI. At doses of 30 and 50 mg/kg orally, MN-001 produces significant protection against the OA-induced bladder hyperactivity. MN-001 might have a role in managing mast cell activity and the associated bladder symptoms in patients with interstitial cystitis.

Gateways to clinical trials

Gateways to Clinical Trials is a guide to the most recent clinical trials in current literature and congresses. The data in the following tables have been retrieved from the Clinical Trials Knowledge Area of Prous Science Integrity, the drug discovery and development portal, http://integrity.prous.com. This issue focuses on the following selection of drugs: Abiraterone acetate, acyline, adalimumab, adenosine triphosphate, AEE-788, AIDSVAX gp120 B/B, AK-602, alefacept, alemtuzumab, alendronic acid sodium salt, alicaforsen sodium, alprazolam, amdoxovir, AMG-162, aminolevulinic acid hydrochloride, aminolevulinic acid methyl ester, aminophylline hydrate, anakinra, anecortave acetate, anti-CTLA-4 MAb, APC-8015, aripiprazole, aspirin, atazanavir sulfate, atomoxetine hydrochloride, atorvastatin calcium, atrasentan, AVE-5883, AZD-2171; Betamethasone dipropionate, bevacizumab, bimatoprost, biphasic human insulin (prb), bortezomib, BR-A-657, BRL-55730, budesonide, busulfan; Calcipotriol, calcipotriol/betamethasone dipropionate, calcium folinate, capecitabine, capravirine, carmustine, caspofungin acetate, cefdinir, certolizumab pegol, CG-53135, chlorambucil, ciclesonide, ciclosporin, cisplatin, clofarabine, clopidogrel hydrogensulfate, clozapine, co-trimoxazole, CP-122721, creatine, CY-2301, cyclophosphamide, cypher, cytarabine, cytolin; D0401, darbepoetin alfa, darifenacin hydrobromide, DASB, desipramine hydrochloride, desloratadine, desvenlafaxine succinate, dexamethasone, didanosine, diquafosol tetrasodium, docetaxel, doxorubicin hydrochloride, drotrecogin alfa (activated), duloxetine hydrochloride, dutasteride; Ecallantide, efalizumab, efavirenz, eletriptan, emtricitabine, enfuvirtide, enoxaparin sodium, estramustine phosphate sodium, etanercept, ethinylestradiol, etonogestrel, etonogestrel/ethinylestradiol, etoposide, exenatide; Famciclovir, fampridine, febuxostat, filgrastim, fludarabine phosphate, fluocinolone acetonide, fluorouracil, fluticasone propionate, fluvastatin sodium, fondaparinux sodium; Gaboxadol, gamma-hydroxybutyrate sodium, gefitinib, gelclair, gemcitabine, gemfibrozil, glibenclamide, glyminox; Haloperidol, heparin sodium, HPV 16/HPV 18 vaccine, human insulin, human insulin; Icatibant, imatinib mesylate, indium 111 (111In) ibritumomab tiuxetan, infliximab, INKP-100, iodine (I131) tositumomab, IoGen, ipratropium bromide, ixabepilone; L-870810, lamivudine, lapatinib, laquinimod, latanoprost, levonorgestrel, licochalcone a, liposomal doxorubicin, lopinavir, lopinavir/ritonavir, lorazepam, lovastatin; Maraviroc, maribavir, matuzumab, MDL-100907, melphalan, methotrexate, methylprednisolone, mitomycin, mitoxantrone hydrochloride, MK-0431, MN-001, MRKAd5 HIV-1 gag/pol/nef, MRKAd5gag, MVA.HIVA, MVA-BN Nef, MVA-Muc1-IL-2, mycophenolate mofetil; Nelfinavir mesilate, nesiritide, NSC-330507; Olanzapine, olmesartan medoxomil, omalizumab, oral insulin, osanetant; PA-457, paclitaxel, paroxetine, paroxetine hydrochloride, PCK-3145, PEG-filgrastim, peginterferon alfa-2a, peginterferon alfa-2b, perillyl alcohol, pexelizumab, pimecrolimus, pitavastatin calcium, porfiromycin, prasterone, prasugrel, pravastatin sodium, prednisone, pregabalin, prinomastat, PRO-2000, propofol, prostate cancer vaccine; Rasagiline mesilate, rhBMP-2/ACS, rhBMP-2/BCP, rhC1, ribavirin, rilpivirine, ritonavir, rituximab, Ro-26-9228, rosuvastatin calcium, rosuvastatin sodium, rubitecan; Selodenoson, simvastatin, sirolimus, sitaxsentan sodium, sorafenib, SS(dsFv)-PE38, St. John's Wort extract, stavudine; Tacrolimus, tadalafil, tafenoquine succinate, talaglumetad, tanomastat, taxus, tegaserod maleate, telithromycin, tempol, tenofovir, tenofovir disoproxil fumarate, testosterone enanthate, TH-9507, thalidomide, tigecycline, timolol maleate, tiotropium bromide, tipifarnib, torcetrapib, trabectedin, travoprost, travoprost/timolol, treprostinil sodium; Valdecoxib, vardenafil hydrochloride hydrate, varenicline, VEGF-2 gene therapy, venlafaxine hydrochloride, vildagliptin, vincristine sulfate, voriconazole, VRX-496, VX-385; Warfarin sodium; Ximelagatran; Yttrium 90 (90Y) ibritumomab tiuxetan; Zanolimumab, zidovudine.

Observation of spin-polarized surface states on ultrathin bct Mn(001) films by spin-polarized scanning tunneling spectroscopy

We report the observation of a magnetic contrast of up to 20% in the scanning tunneling spectroscopy dI/dV maps obtained with Fe-coated tips on Mn(001) layers grown on an Fe(001) whisker at 370 K. These nanometer resolution microscopy results show that the layers couple antiferromagnetically. By normalizing the dI/dV curves by tunneling probability functions, we found a spin-dependent peak on the body-centered-tetragonal (bct) Mn(001) surface at +0.8 V, whose high spin polarization gives rise to the dI/dV map contrast. Band structure calculations allow one to identify the +0.8 V peak as due to two spin-polarized d(z(2)) surface states.

Single molecule magnetoresistance with combined antiferromagnetic and ferromagnetic electrodes

The magnetoresistance of a hydrogen-phthalocyanine molecule placed on an antiferromagnetic Mn(001) surface and contacted by a ferromagnetic Fe electrode is investigated using density functional theory based transport calculations and low-temperature scanning tunneling microscopy. A large and negative magnetoresistance ratio of ~50% is observed in combination with a high conductance. The effect originates from a lowest unoccupied molecular orbital (LUMO) doublet placed almost in resonance with the Fermi energy. As a consequence, irrespective of the mutual alignment of magnetizations, electron transport is always dominated by resonant transmission of Mn-majority charge carries going through LUMO levels.