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Laquinimod
別名：ABR-215062, LAQ
Laquinimod (ABR-215062, LAQ) is a potent immunomodulator. Phase 3.
CAS No. 248281-84-7
文献中Selleckの製品使用例（2）
製品安全説明書
現在のバッチを見る：
S278701
DMSO]
61 mg/mL]
false]
Ethanol]
1 mg/mL]
false]
Water]
Insoluble]
false
純度：
99.96%
99.96
Laquinimod関連製品
Immunology & Inflammation related阻害剤の選択性比較
生物活性
| 製品説明 | Laquinimod (ABR-215062, LAQ) is a potent immunomodulator. Phase 3. |
|---|
| In Vitro | ||||
| In vitro | Laquinimod treatment at 0.1-1 μM does not affect the viability of peripheral blood mononuclear cells (PBMC). By performing the large-scale gene expression microarray analysis in PBMC from healthy subjects or relapsing-remitting multiple sclerosis (RRMS) patients, Laquinimod is shown to induce suppression of genes related to antigen presentation and corresponding inflammatory pathways. Laquinimod induces activation of Th2 response in CD14+ and CD4+ cells and suppression of proliferation in CD8+ cells. Laquinimod displays significant effects on immune modulation related to the suppression of antigen presenting mechanism followed by a decrease of chemotaxis and adhesion, and exhibits potent anti-inflammatory potency through the suppression of the NF-κB pathway that concordantly leads to the activation of apoptosis of immuno-competent cells. [5] | |||
|---|---|---|---|---|
| 細胞実験 | 細胞株 | PBMC | ||
| 濃度 | Dissolved in PBS, final concentrations ~1 μM | |||
| 反応時間 | 24 hours | |||
| 実験の流れ | The peripheral blood mononuclear cells (PBMC) are incubated with Laquinimod for 24 hours. Cell viability is measured on total PBMC by propidium iodide (PI) staining using an automated cell counter. Protein expression level is assessed in PBMC samples by Western blot using anti-HLA-DQA/DQB monoclonal antibodies. | |||
| In Vivo | ||
| In Vivo | Administration of Laquinimod (0.16-16 mg/kg/day) dose-dependently inhibits the incidence of experimental autoimmune neuritis (EAN) in Lewis rats, ameliorates clinical signs and inhibits P0 peptide 180-199-specific T cell responses as well as the inflammation and demyelination in the peripheral nerves, suggesting that Laquinimod may mediate its effects by regulation of Th1/Th2 cytokine balance. [1] Laquinimod significantly inhibits the development of murine acute experimental autoimmune encephalomyelitis (EAE), being approximately 20 times more potent than the immunomodulator roquinimex. [2] Laquinimod treatment inhibits the development of experimental autoimmune encephalomyelitis (EAE) in the Lewis rat in a dose-dependent manner, and shows better disease inhibitory effects as compared to roquinimex (Linomide). [3] Laquinimod potently inhibits the development of chronic experimental autoimmune encephalomyelitis (chEAE) in IFN-beta k.o. mice and wild type mice. [4] Laquinimod reduces clinical signs, inflammation, and demyelination in C57BL/6 mice with active EAE induced with MOG(35-55) peptide, and down-regulates VLA-4-mediated adhesiveness and pro-inflammatory cytokines such as IL-17. [6] The study of Laquinimod in the mice model of EAE using a conditional BDNF knockout strain lacking BDNF expression in myeloid cells and T cells (LLF mice) indicates Laquinimod also modulates autoimmune demyelination via induction of brain-derived neurotrophic factor (BDNF). [7] | |
|---|---|---|
| 動物実験 | 動物モデル | Lewis rats with experimental autoimmune neuritis (EAN) induced by inoculation with peripheral nerve myelin P0 protein peptide 180-199 and Freund's complete adjuvant |
| 投与量 | 0.16, 1.6 and 16 mg/kg/day | |
| 投与経路 | Administered via a daily subcutaneous injection | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT06161415 | Recruiting | Inflammation|Uveitis |
Quan Dong Nguyen|Global Ophthalmic Research Center (GORC)|Stanford University |
April 2024 | Phase 1 |
| NCT05187403 | Completed | Eye Diseases |
Active Biotech AB |
December 9 2021 | Phase 1 |
| NCT02772523 | Completed | Alzheimer''s Disease |
Barcelonabeta Brain Research Center Pasqual Maragall Foundation |
May 2016 | Not Applicable |
| NCT02085863 | Completed | Pharmacokinetics|Pharmacodynamics |
Teva Branded Pharmaceutical Products R&D Inc. |
February 2014 | Phase 1 |
| NCT01975298 | Withdrawn | Relapsing Remitting Multiple Sclerosis |
Teva Branded Pharmaceutical Products R&D Inc. |
January 2014 | Phase 3 |
化学情報
| 分子量 | 356.8 | 化学式 | C19H17ClN2O3 |
| CAS No. | 248281-84-7 | SDF | Download Laquinimod SDFをダウンロードする |
| Smiles | CCN(C1=CC=CC=C1)C(=O)C2=C(C3=C(C=CC=C3Cl)N(C2=O)C)O | ||
| 保管 | |||
|
In vitro |
DMSO : 61 mg/mL ( (170.96 mM)； 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。) Ethanol : 1 mg/mL Water : Insoluble |
モル濃度計算器 |
|
in vivo Add solvents to the product individually and in order. |
投与溶液組成計算機 | ||||
実験計算
投与溶液組成計算機(クリア溶液)
ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）
mg/kg
g
μL
匹
ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結果：
投与溶媒濃度： mg/ml;
DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )
投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH2O，を加え完全に溶解させます。
投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。
注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。
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