2. GPCR/G Protein
  3. LPL Receptor
  4. Ozanimod

Ozanimod  (Synonyms: RPC-1063)

製品番号: HY-12288 純度: 99.88%
COA 取扱説明書

Molarity Calculator

Ozanimod (RPC-1063), a sphingosine 1-phosphate (S1P) receptor modulator that binds with high affinity selectively to S1P receptor subtypes 1 (S1P1) and 5 (S1P5). Ozanimod has modulate effect for hS1P1 and hS1P5 receptor with EC50s of 1.03 nM and 8.6 nM, respectively. Ozanimod can be used for the research of relapsing multiple sclerosis (MS).

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Ozanimod 構造式

Ozanimod 構造式

CAS 番号 : 1306760-87-1

容量 価格（税別） 在庫状況 数量
無料サンプル (0.1 - 0.5 mg)   今すぐ申し込む  
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 132 在庫あり
Solution
10 mM * 1 mL in DMSO USD 132 在庫あり
Solid
5 mg USD 120 在庫あり
10 mg USD 180 在庫あり
25 mg USD 370 在庫あり
50 mg USD 580 在庫あり
100 mg USD 850 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

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Based on 2 publication(s) in Google Scholar

Other Forms of Ozanimod:

Ozanimod 関連抗体

Top Publications Citing Use of Products

LPL Receptor アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
LPAR1 LPAR2 LPAR3 LPAR5 S1PR1 S1PR2 S1PR3 S1PR4 S1PR5

  • 生物活性

  • 純度とドキュメンテーション

  • 参考文献

  • カスタマーレビュー

製品説明

Ozanimod (RPC-1063), a sphingosine 1-phosphate (S1P) receptor modulator that binds with high affinity selectively to S1P receptor subtypes 1 (S1P1) and 5 (S1P5). Ozanimod has modulate effect for hS1P1 and hS1P5 receptor with EC50s of 1.03 nM and 8.6 nM, respectively. Ozanimod can be used for the research of relapsing multiple sclerosis (MS)[1].

IC50 & Target

S1PR1

1.03 nM (EC50)

S1PR5

8.6 nM (EC50)

体外実験

Ozanimod (RPC-1063) has potency and intrinsic activity of S1P receptor modulators for S1P5 across species with [35S]-GTPgS binding, and the EC50 values of 1.03 nM, 1.29 nM, 0.90 nM, 1.02 nM and 0.61 nM for Human S1P1, Cynomolgus monkey S1P1, Mouse S1P1, Rat S1P1 and Canine S1P1, respectively; and the EC50 values of 8.6 nM, 15.9 nM, 957.5 nM, 2032.7 nM and 1662.0 nM for Human S1P5, Cynomolgus monkey S1P5, Mouse S1P5, Rat S1P5 and Canine S1P5, respectively[1].
Ozanimod restores the potency with EC50 from 958 nM for mS1P5 to 6.7 nM for mS1P5_A120T to closely mirror the EC50 for hS1P5 of 8.6 nM by mutating the alanine in the mouse sequence[1].
Ozanimod has binding affinity with Ki values of 2.0 nM, 59.9 nM and 5.6 nM for hS1P5, mS1P5 and mS1P5 _A120T, respectively[1].
Ozanimod has saturation binding of [3H]-ozanimod to hS1P5, and mS1P5_A120T with KD values of 6.56 nM, 7.35 nM, respectively and also has saturation binding for [3H]-A971432 to S1P5D value of 8.75 nM[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Ozanimod 関連抗体
体内実験

Ozanimod (RPC-1063) (oral gavage; 0.05, 0.2, or 1 mg/kg; once daily; for 14 consecutive days) exposures sufficient to engage S1P1, but not S1P5, results in reduced circulating lymphocytes, disease scores, and body weight loss; reduces inflammation, demyelination, and apoptotic cell counts in the spinal cord; and reduces circulating levels of the neuronal degeneration marker, neurofilament light[1].
Ozanimod (oral gavage; 5 mg/kg; once-daily) prevents axonal degradation and myelin loss during toxin challenge but does not facilitate enhanced remyelination after intoxication[1].
Ozanimod (oral, 1 or 5 mg/kg, for 7 days) has good pharmacokinetics in mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Experimental Autoimmune Encephalomyelitis Model[1]
Dosage: 0.05, 0.2, or 1 mg/kg
Administration: oral gavage; 0.05, 0.2, or 1 mg/kg; once daily; for 14 consecutive days
Result: Attenuated body weight loss, terminal disease scores were significantly attenuated with the 0.2 and 1 mg/kg doses and ALCs were significantly reduced in all dose groups.
Reduced spinal cord inflammation and demyelination, as well as attenuated the number of spinal cord apoptotic cells, and significantly reduced the levels of circulating neurofilament light at the top dose of 1 mg/kg.
Animal Model: Cuprizone/Rapamycin Demyelination Model[1]
Dosage: 5 mg/kg
Administration: oral gavage; 5 mg/kg; once-daily
Result: Protected neuronal axons, preventing breakage and ovoid formation in the corpus callosum of CPZ/Rapa treated mice.
Significantly attenuated the extent to which the corpus callosum demonstrated reduced myelin content as visualized by MRI.
Did not result in enhanced myelin content.
Animal Model: C57BL/6J mice[1]
Dosage: 1 or 5 mg/kg
Administration: oral, 1 or 5 mg/kg, for 7 days
Result:
Dose Terminal body weight % versus day 1 Spinal cord inflammation Foci per 20 cells Spinal cord demyelination Score 0–5 Spinal cord apoptotic cells Count per section Plasma NfL pg/ml
Vehicle (5% DMSO, 5%Tween 20, 90% water) 86.4 ± 3.2 8.50 ± 1.21 2.00 ± 0.15 2.25 ± 0.53 4.37 ± 0.89
Ozanimod (0.05 mg/kg) 85.8 ± 2.7 5.00 ± 1.03* 0.91 ± 0.21*** 1.08 ± 0.23* 3.53 ± 0.46
Ozanimod (0.2 mg/kg) 95.7 ± 3.1* 3.54 ± 0.49*** 0.73 ± 0.14 *** 0.91 ± 0.28* 2.62 ± 0.46
Ozanimod (1 mg/kg) 102.8 ± 1.8* 2.67 ± 0.56*** 0.33 ± 0.14 *** 0.60 ± 0.19** 1.91 ± 0.34**
臨床実験
分子量

404.46

分子式

C23H24N4O3
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

N#CC1=CC(C2=NC(C3=CC=CC4=C3CC[C@@H]4NCCO)=NO2)=CC=C1OC(C)C
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : ≥ 29 mg/mL (71.70 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4724 mL 12.3622 mL 24.7243 mL
5 mM 0.4945 mL 2.4724 mL 4.9449 mL
10 mM 0.2472 mL 1.2362 mL 2.4724 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.18 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (6.18 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション

純度: 99.88%

COA (253 KB) HNMR (263 KB) LCMS (94 KB)

取扱説明書 (2659 KB)
参考文献

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4724 mL 12.3622 mL 24.7243 mL 61.8108 mL
5 mM 0.4945 mL 2.4724 mL 4.9449 mL 12.3622 mL
10 mM 0.2472 mL 1.2362 mL 2.4724 mL 6.1811 mL
15 mM 0.1648 mL 0.8241 mL 1.6483 mL 4.1207 mL
20 mM 0.1236 mL 0.6181 mL 1.2362 mL 3.0905 mL
25 mM 0.0989 mL 0.4945 mL 0.9890 mL 2.4724 mL
30 mM 0.0824 mL 0.4121 mL 0.8241 mL 2.0604 mL
40 mM 0.0618 mL 0.3091 mL 0.6181 mL 1.5453 mL
50 mM 0.0494 mL 0.2472 mL 0.4945 mL 1.2362 mL
60 mM 0.0412 mL 0.2060 mL 0.4121 mL 1.0302 mL
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Ozanimod Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Ozanimod1306760-87-1RPC-1063RPC1063RPC 1063LPL ReceptorLysophospholipid Receptorsphingosine 1-phosphate (S1P)S1P receptor subtypes 1 (S1P1)S1P receptor subtypes 5 (S1P5)multiple sclerosis (MS)neurosurgeryInhibitorinhibitorinhibit

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製品名:
Ozanimod
製品番号:
HY-12288
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