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BAF-312(SiponiMod)

Product Name
BAF-312(SiponiMod)
CAS No.
1230487-00-9
Chemical Name
BAF-312(SiponiMod)
Synonyms
SiponiMod;Siponimod (BAF-312);SIPONIMOD; SIPONIMOD [INN]; BAF-312; BAF 312;(E)-1-(4-(1-(4-cyclohexyl-3-(trifluoromethyl)benzyloxyimino)ethyl)-2-ethylbenzyl)azetidine-3-carboxylic acid;CS-1753;Sinimod;Siponimod D11;D11-Siponimod;Siponimod [INN];BAF-312(SiponiMod)
CBNumber
CB62725945
Molecular Formula
C29H35F3N2O3
Formula Weight
516.59
MOL File
1230487-00-9.mol
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BAF-312(SiponiMod) Property

Melting point:
154 - 157°C
Boiling point:
602.0±65.0 °C(Predicted)
Density 
1.24±0.1 g/cm3(Predicted)
storage temp. 
Hygroscopic, Refrigerator, under inert atmosphere
solubility 
DMSO (Slightly), Methanol (Slightly)
pka
2.69±0.20(Predicted)
form 
Solid
color 
White to Off-White
InChIKey
KIHYPELVXPAIDH-HNSNBQBZSA-N
SMILES
N1(CC2=CC=C(/C(=N/OCC3=CC=C(C4CCCCC4)C(C(F)(F)F)=C3)/C)C=C2CC)CC(C(O)=O)C1
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML3830
Product name
BAF312
Purity
≥98% (HPLC)
Packaging
10mg
Price
$102
Updated
2025/07/31
Sigma-Aldrich
Product number
SML3830
Product name
BAF312
Purity
≥98% (HPLC)
Packaging
50mg
Price
$328
Updated
2025/07/31
Cayman Chemical
Product number
22057
Product name
Siponimod
Purity
≥98%
Packaging
1mg
Price
$32
Updated
2024/03/01
Cayman Chemical
Product number
22057
Product name
Siponimod
Purity
≥98%
Packaging
5mg
Price
$131
Updated
2024/03/01
Cayman Chemical
Product number
22057
Product name
Siponimod
Purity
≥98%
Packaging
10mg
Price
$230
Updated
2024/03/01
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BAF-312(SiponiMod) Chemical Properties,Usage,Production

Description

S1p signaling is important for immune, cardiovascular, and CNS function.Like its FDA approved predecessor fingolimod, siponimod is an oral S1p signaling modulator.While fin- golimod binds four out of five known S1p receptors, siponimod is selective for receptor sub- types 1 and 5. This selectivity may allow for an improved adverse event profile.

Uses

Siponimod is a functional sphingosine -1 phosphate (SIP) antagonist used in the treatment of multiple sclerosis and other central nervous system-related diseases in human subjects. .

Side effects

Siponimod,2 mg/day, was studied in a Phase I placebo-controlled trial in patients with secondary progressive Ms.206The primary endpoint was time to 3 months confirmed dis- ability progression. There were substantive side effects from the drug，mainly increased liver transaminase concentrations,bradycardia, and bradyarrhythmia at treatment initiation.With subsequent siponimod administration，there was an increased incidence of macular edema, hypertension,varicella zoster reactivation, and convulsions compared to placebo. By grad- ually escalating the initial dose of siponimod, cardiac first-dose effects were reduced.While the results of this trial are encouraging,long- term safety issues may be a greater concern5or since persons with secondary progressive MS as a group are older,with a higher incidence of comorbidities that could preclude use of siponimod.

Synthesis

Synthesis of BAF-312(SiponiMod)


in vivo

Siponimod (1 g/kg; i.v.; single dose) shows low to moderate in monkey, but high in rat in metabolism studies with liver microsomes. The absolute bioavailability is 50 and 71% in the rat and monkey, respectively, indicating no major presystemic first pass metabolism[1].
Siponimod (0.3, 3 mg/kg; p.o.; once daily; 23 d) suppresses experimental autoimmune encephalomyelitis (EAE) in rats by internalizing S1P1 receptors[2].
Parmacokinetics of Siponimod in rats and monkey[1]

/td> CL (L/h/kg)Vss (L/kg)T1/2 (h)F (%)
Rat0.362.15650
Monkey0.098/td> 2.121971
Animal Model:Experimental autoimmune encephalomyelitis (EAE) model in Lewis rats (200-250 g)[2]
Dosage:0.03, 0.3, 3 mg/kg
Administration:Oral gavage; once daily; 23 days
Result:Decreased peripheral lymphocyte counts by 88% at the Tmax of 8 h postadministration.

target

S1P1 receptors

IC 50

S1PR1: 0.39 nM (EC50); S1PR5: 0.98 nM (EC50); S1PR4: 750 nM (EC50); S1PR3: >1000 nM (EC50); S1PR2: >10000 nM (EC50)

References

[1] gergely p1, nuesslein-hildesheim b, guerini d, brinkmann v, traebert m, bruns c, pan s, gray ns, hinterding k, cooke ng, groenewegen a, vitaliti a, sing t, luttringer o, yang j, gardin a, wang n, crumb wj jr, saltzman m, rosenberg m, wallström e. the selective sphingosine 1-phosphate receptor modulator baf312 redirects lymphocyte distribution and has species-specific effects on heart rate. br j pharmacol. 2012 nov;167(5):1035-47.
[2] pan s1, gray ns1, gao w1, mi y1, fan y1, wang x1, tuntland t1, che j1, lefebvre s1, chen y1, chu a1, hinterding k2, gardin a2, end p2, heining p2, bruns c2, cooke ng2, nuesslein-hildesheim b2 .discovery of baf312 (siponimod), a potent and selective s1p receptor modulator. acs med chem lett. 2013 jan 4;4(3):333-7.

BAF-312(SiponiMod) Preparation Products And Raw materials

Raw materials

Preparation Products

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BAF-312(SiponiMod) Suppliers

China 189 India 6 United Kingdom 1 United States 11 Global 207
Shanghai Zhengyi Pharmaceutical Co., Ltd
Tel
17740884366
Email
derek1229@163.com
Country
China
ProdList
61
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58
Hunan Revel Biotechnology Co. , Ltd.
Tel
19359985961
Email
2430503320@qq.com
Country
China
ProdList
1452
Advantage
58
Shijiazhuang Dingmin pharmaceutical Sciences Co.,Ltd
Tel
0311-67591193 15030197620
Fax
QQ:2786999724
Email
sales02@dingminpharma.com
Country
China
ProdList
255
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58
Hubei wei shi reagent group ltd., company
Tel
027-59102966 18717199209
Email
2853877583@QQ.com
Country
China
ProdList
7498
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58
Dalian Meilun Biotech Co., Ltd.
Tel
0411-62910999 13889544652
Email
sales@meilune.com
Country
China
ProdList
4747
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58
Haoyuan Chemexpress Co., Ltd.
Tel
021-58950125
Fax
(86) 21-58955996
Email
info@chemexpress.com
Country
China
ProdList
7552
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61
Nanjing Sunlida Biological Technology Co., Ltd.
Tel
025-57798810
Fax
025-57019371
Email
sales@sunlidabio.com
Country
China
ProdList
3239
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55
TargetMol Chemicals Inc.
Tel
021-021-33632979 15002134094
Fax
021-33632979
Email
marketing@targetmol.com
Country
China
ProdList
7782
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58
ShangHai Caerulum Pharma Discovery Co., Ltd.
Tel
18149758185
Email
sales-cpd@caerulumpharma.com
Country
China
ProdList
3506
Advantage
58
Hygeia (Chengdu) pharmaceutical technique Co., Ltd
Tel
028-84502008 13568869383
Fax
028-66476329
Email
sales@hygeiapharm.com
Country
China
ProdList
296
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55
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View Lastest Price from BAF-312(SiponiMod) manufacturers

Wuhan Haorong Biotechnology Co.,Ltd
Product
BAF-312(SiponiMod) 1230487-00-9
Price
US $0.00-0.00/KG
Min. Order
1KG
Purity
99%
Supply Ability
5000
Release date
2023-08-07
Wuhan Nutra Biotechnology Co.,Ltd
Product
SiponiMod; BAF-312 1230487-00-9
Price
US $0.00-0.00/g
Min. Order
1g
Purity
98%
Supply Ability
10kgs
Release date
2021-05-23
Hangzhou ICH Biofarm Co., Ltd
Product
BAF-312(SiponiMod) 1230487-00-9
Price
US $0.00-0.00/kg
Min. Order
0.10000000149011612kg
Purity
99.0%min
Supply Ability
200kg
Release date
2023-06-12

1230487-00-9, BAF-312(SiponiMod)Related Search:

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  • BAF-312(SiponiMod)
  • SiponiMod
  • 3-Azetidinecarboxylic acid, 1-[[4-[(1E)-1-[[[4-cyclohexyl-3-(trifluoromethyl)phenyl]methoxy]imino]ethyl]-2-ethylphenyl]methyl]-
  • 1-(4-[1-[(E)-4-Cyclohexyl-3-trifluoromethyl-benzyloxyimino]-ethyl]-2-ethyl-benzyl)-azetidine-3-carboxylic acid
  • (E)-1-(4-(1-(4-cyclohexyl-3-(trifluoromethyl)benzyloxyimino)ethyl)-2-ethylbenzyl)azetidine-3-carboxylic acid
  • BAF312 (Siponimod) 1-[[4-[(E)-N-[[4-cyclohexyl-3-(trifluoromethyl)phenyl]methoxy]-C-methylcarbonimidoyl]-2-ethylphenyl]methyl]azetidine-3-carboxylic acid
  • Siponimod (BAF-312)
  • Siponimod [INN]
  • SIPONIMOD; SIPONIMOD [INN]; BAF-312; BAF 312
  • CS-1753
  • BAF-312(SiponiMod) USP/EP/BP
  • Siponimod D11
  • 1-[[4-[(E)-N-[[4-cyclohexyl-3-(trifluoromethyl)phenyl]methoxy]-C-methylcarbonimidoyl]-2-ethylphenyl]methyl]azetidine-3-carboxylic acid
  • Formyl sitagliptin d4
  • Sinimod
  • Siponimod, 10 mM in DMSO
  • D11-Siponimod
  • 1230487-00-9
  • C29H35F3N2O3
  • API
  • Inhibitors