Referencia número: HY-16989

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SR9009

39 Cited Publications

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Based on 39 publication(s) in Google Scholar

SR9009 is a REV-ERBα/β agonist with IC₅₀s of 670 nM and 800 nM for REV-ERBα and REV-ERBβ, respectively.

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Pureza: 99.32%
No. CAS: 1379686-30-2
Fòrmula: C₂₀H₂₄ClN₃O₄S
Peso molecular:437.94

Almacenamiento:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

SR9009 Chemical Structure

No. CAS: 1379686-30-2

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (39)
Solvente y solubilidad
- In Vitro
- In Vivo
Protocolo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

SR9009 is a REV-ERBα/β agonist with IC₅₀s of 670 nM and 800 nM for REV-ERBα and REV-ERBβ, respectively.

IC₅₀ & Target

IC50: 670 nM (Rev-ErbBα), 800 nM (Rev-ErbBβ)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	EC₅₀	0.7 μM Compound: 12e	Agonist activity at Rev-Erbalpha expressed in HEK293 cells coexpressing BamII promoter assessed as repression of transcription after 24 hrs by dual-Glo luciferase assay Agonist activity at Rev-Erbalpha expressed in HEK293 cells coexpressing BamII promoter assessed as repression of transcription after 24 hrs by dual-Glo luciferase assay	[PMID: 22633688]
HEK293	IC₅₀	670 nM Compound: 12e	Agonist activity at Rev-Erbalpha expressed in HEK293 cells coexpressing Gal4 ligand binding domain assessed as inhibition of transcription after 24 hrs by dual-Glo luciferase assay Agonist activity at Rev-Erbalpha expressed in HEK293 cells coexpressing Gal4 ligand binding domain assessed as inhibition of transcription after 24 hrs by dual-Glo luciferase assay	[PMID: 22633688]
HEK293	IC₅₀	670 nM Compound: SR9009	Increased REV-ERB-alpha LBD dependent repressor activity in HEK293 cell reporter assay Increased REV-ERB-alpha LBD dependent repressor activity in HEK293 cell reporter assay	[PMID: 22460951]
HEK293	IC₅₀	710 nM Compound: SR9009	REV-ERB-alpha mediated transcriptional suppression at Bmal1 promoter in HEK293 cell reporter assay REV-ERB-alpha mediated transcriptional suppression at Bmal1 promoter in HEK293 cell reporter assay	[PMID: 22460951]
HEK293	IC₅₀	800 nM Compound: SR9009	Increased REV-ERB-beta LBD dependent repressor activity in HEK293 cell reporter assay Increased REV-ERB-beta LBD dependent repressor activity in HEK293 cell reporter assay	[PMID: 22460951]

In Vitro

SR9009 dose-dependently increases the REV-ERB-dependent repressor activity assessed in HEK293 cells expressing a chimeric Gal4 DNA Binding Domain (DBD)-REV-ERB ligand binding domain (LBD)α or β and a Gal4-responsive luciferase reporter (SR9009: REV-ERBα IC₅₀=670 nM, REV-ERBβ IC₅₀=800 nM). SR9009 potently and efficaciously suppresses transcription in a cotransfection assay using full-length REV-ERBα along with a luciferase reporter driven by the Bmal1 promoter (IC₅₀=710 nM). SR9009 suppresses the expression of BMAL1 mRNA in HepG2 cells in a REV-ERBα/β-dependent manner. Direct binding of the SR9009 to REV-ERBα is also confirmed using circular dichrosim analysis (K_d=800 nM)^[1].

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

In Vivo

SR9009 (100 mg/kg ,i.p.) treated mice exhibit a more severe reduction in adiposity. Plasma non-esterified fatty acids (NEFA) are also reduced (23%) along with plasma glucose (19%) in the SR9009 treated animals. In the white adipose tissue (WAT) , SR9009 treatment results in a decrease in expression of genes encoding enzymes involved in triglyceride (TG) synthesis as is also observed in lean mice^[1].

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

Chemical Information

No. CAS 1379686-30-2
Appearance Solid
Peso molecular 437.94
Fòrmula C₂₀H₂₄ClN₃O₄S
Color White to off-white
SMILES

O=C(N1CC(CN(CC2=CC=C(Cl)C=C2)CC3=CC=C([N+]([O-])=O)S3)CC1)OCC
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (39)

All WBCell Proliferation/Viability Assay

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Journal Impact Factor

J Hepatol

Targeting the liver clock improves fibrosis by restoring TGF-β signaling. [Abstract]

2025 Jan;82(1):120-133. PMID: 39173955
Nat Metab

Cellular Feimin enhances exercise performance by suppressing muscle thermogenesis. [Abstract]

2025 Jan;7(1):84-101. PMID: 39747484
Cancer Res

Disrupting Circadian Rhythm via the PER1-HK2 Axis Reverses Trastuzumab Resistance in Gastric Cancer. [Abstract]

2022 Apr 15;82(8):1503-1517. PMID: 35255118
Nat Commun

Deficiency of intestinal Bmal1 prevents obesity induced by high-fat feeding. [Abstract]

2021 Sep 7;12(1):5323. PMID: 34493722
Nat Commun

REV-ERBα integrates colon clock with experimental colitis through regulation of NF-κB/NLRP3 axis. [Abstract]

2018 Oct 12;9(1):4246. PMID: 30315268

SR9009 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2018 Oct 12;9(1):4246. [Abstract]

Western blotting of peritoneal macrophages (PMs) after co-treatment of SR9009 (for 12 h) and LPS/ATP. LPS is added before or after SR9009 treatment for 3 h, followed by ATP addition for 30 min (added last).
Cell Discov

Chronobiology of neurotropic viruses: rhythmic viral entry and arrhythmic host clocks. [Abstract]

2026 Feb 10;12(1):11. PMID: 41663379
J Biomed Sci

Circadian gene Rev-erbα influenced by sleep conduces to pregnancy by promoting endometrial decidualization via IL-6-PR-C/EBPβ axis. [Abstract]

2022 Nov 24;29(1):101. PMID: 36419076
Cell Death Differ

Developmental growth plate cartilage formation suppressed by artificial light at night via inhibiting BMAL1-driven collagen hydroxylation. [Abstract]

2023 Jun;30(6):1503-1516. PMID: 37029304
Cell Death Dis

SR9009 inhibits lethal prostate cancer subtype 1 by regulating the LXRα/FOXM1 pathway independently of REV-ERBs. [Abstract]

2022 Nov 10;13(11):949. PMID: 36357378

SR9009 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2022 Nov 10;13(11):949. [Abstract]

SR9009 (0-50 μM; 48 h) markedly inhibits 22RV1, PC3 and DU145 cell viability in a dose-dependent manner but had no impact on RWPE-1 cells.
J Neuroinflammation

The circadian clock protein Rev-erbα provides neuroprotection and attenuates neuroinflammation against Parkinson's disease via the microglial NLRP3 inflammasome. [Abstract]

2022 Jun 6;19(1):133. PMID: 35668454
J Neuroinflammation

Decreased expression of Rev-Erbα in the epileptic foci of temporal lobe epilepsy and activation of Rev-Erbα have anti-inflammatory and neuroprotective effects in the pilocarpine model. [Abstract]

2020 Jan 31;17(1):43. PMID: 32005256
J Orthop Translat

Inhibiting the REV-ERBα expression protects against mechanical overloading-induced cartilage clock disruption and osteoarthritis progression. [Abstract]

2025 Jun 18:53:112-125. PMID: 40606845
Int J Mol Med

Melatonin inhibits RANKL‑induced osteoclastogenesis through the miR‑882/Rev‑erbα axis in Raw264.7 cells. [Abstract]

2021 Feb;47(2):633-642. PMID: 33416111
Cell Rep

IRE1α regulates macrophage phagocytosis in immune thrombocytopenia through NR1D1 mRNA decay and lysosomal biogenesis. [Abstract]

2026 Mar 12;45(3):117083. PMID: 41824452
Cell Rep

Genetic or pharmacologic blockade of mPGES-2 attenuates renal lipotoxicity and diabetic kidney disease by targeting Rev-Erbα/FABP5 signaling. [Abstract]

2024 Apr 23;43(4):114075. PMID: 38583151
Aging Cell

Identification of a small molecule SR9009 that activates NRF2 to counteract cellular senescence. [Abstract]

2021 Oct;20(10):e13483. PMID: 34587364
Cell Prolif

Circadian clock genes promote glioma progression by affecting tumour immune infiltration and tumour cell proliferation. [Abstract]

2021 Mar;54(3):e12988. PMID: 33442944
J Pineal Res

Melatonin Ameliorates Circadian Disruption-Associated Dry Eye via Modulation of BMAL1-REV-ERBα-IL-17 Axis and Ocular Surface Microbiota Homeostasis. [Abstract]

2025 Sep;77(5):e70076. PMID: 40936475
Clin Exp Hypertens

Nuclear receptor subfamily 1 group D member 1 suppresses the proliferation, migration of adventitial fibroblasts, and vascular intimal hyperplasia via mammalian target of rapamycin complex 1/β-catenin pathway. [Abstract]

2023 Dec 31;45(1):2178659. PMID: 36794491
Biochem Pharmacol

Circadian pharmacological effects of berberine on chronic colitis in mice: Role of the clock component Rev-erbα. [Abstract]

2020 Feb:172:113773. PMID: 31866303
Int Endod J

Rev-erbα attenuates refractory periapical periodontitis via M1 polarization: An in vitro and in vivo study. [Abstract]

2024 Apr;57(4):451-463. PMID: 38279698
Inflamm Res

Arntl deficiency impairs NK cell function by reducing responsiveness to IL-15 and suppressing activation. [Abstract]

2026 Jun 8;75(1):136. PMID: 42257758
EMBO Rep

Genetic disruption of the circadian gene Bmal1 in the intestinal epithelium reduces colonic inflammation. [Abstract]

2025 Apr 30. PMID: 40307620
Eur J Pharmacol

7,8-Dihydroxyflavone alleviates cardiac fibrosis by restoring circadian signals via downregulating Bmal1/Akt pathway. [Abstract]

2023 Jan 5:938:175420. PMID: 36427535
Int Immunopharmacol

Berberine alleviates LPS-induced inflammatory response by targeted activation of NR1D1 in bovine endometrial epithelial cells. [Abstract]

2026 Aug 15:183:116858. PMID: 42150288
J Cell Mol Med

Melatonin inhibits osteoclastogenesis via RANKL/OPG suppression mediated by Rev-Erbα in osteoblasts. [Abstract]

2022 Jul;26(14):4032-4047. PMID: 35726597
ACS Chem Neurosci

Nr1d1 Regulates Microglia M1/M2 Polarization to Alleviate Neuroinflammation after Traumatic Brain Injury. [Abstract]

2025 Nov 26. PMID: 41296614
iScience

Glucocorticoid receptor-mediated Nr1d1 chromatin circadian misalignment in stress-induced irritable bowel syndrome. [Abstract]

2023 Jun 17;26(7):107137. PMID: 37404374
Acta Biochim Biophys Sin (Shanghai)

Activation of Rev-erbα attenuates lipopolysaccharide-induced inflammatory reactions in human endometrial stroma cells via suppressing TLR4-regulated NF-κB activation. [Abstract]

2019 Sep 6;51(9):908-914. PMID: 31411318
J Pharm Biomed Anal

Screening method of mildronate and over 300 doping agents by reversed-phase liquid chromatography-high resolution mass spectrometry. [Abstract]

2021 Feb 20:195:113870. PMID: 33453569
Drug Test Anal

High-throughput liquid chromatography tandem mass spectrometry assay as initial testing procedure for analysis of total urinary fraction. [Abstract]

2021 Feb;13(2):283-298. PMID: 32852861
Biochem Biophys Res Commun

REV-ERBs negatively regulate mineralization of the cementoblasts. [Abstract]

2022 Jan 8:587:9-15. PMID: 34861472
Am J Reprod Immunol

Circadian rhythm-associated Rev-erbα modulates polarization of decidual macrophage via the PI3K/Akt signaling pathway. [Abstract]

2021 Sep;86(3):e13436. PMID: 33934423
Cell Physiol Biochem

Angiotensin II Suppresses Rev-erbα Expression in THP-1 Macrophages via the Ang II Type 1 Receptor/Liver X Receptor α Pathway. [Abstract]

2018;46(1):303-313. PMID: 29590657

SR9009 purchased from MedChemExpress. Usage Cited in: Cell Physiol Biochem. 2018;46(1):303-313. [Abstract]

Rev-erbα expression in relation to MMP-9 protein expression is induced by Ang II in THP-1 macrophages. MMP- 9 protein expression is analyzed by western blotting.
Can Respir J

SR9009 Regulates Acute Lung Injury in Mice Induced by Sepsis. [Abstract]

2022 Jul 1:2022:5802938. PMID: 35814267
bioRxiv

2025 June 01.
Heliyon

REV-ERBα inhibitor rescues MPTP/MPP+-induced ferroptosis of dopaminergic neuron through regulating FASN/SCD1 signaling pathway. [Abstract]

2024 Nov 15;10(23):e40388. PMID: 39654780
Oxid Med Cell Longev

NR1D1 Deletion Induces Rupture-Prone Vulnerable Plaques by Regulating Macrophage Pyroptosis via the NF- κ B/NLRP3 Inflammasome Pathway. [Abstract]

2021 Dec 16:2021:5217572. PMID: 34956438
Chemosphere

Bisphenol A attenuates testosterone production in Leydig cells via the inhibition of NR1D1 signaling. [Abstract]

2021 Jan:263:128020. PMID: 33297044

SR9009 purchased from MedChemExpress. Usage Cited in: Chemosphere. 2021 Jan:263:128020. [Abstract]

SR9009 administration remarkably increases the protein expression levels of NR1D1 at both 24 and 48 h, while attenuating the protein expression levels of BMAL1. The protein expression levels of StAR are also elevated at 24 h.

Solvente y solubilidad

In Vitro:

DMSO : ≥ 100 mg/mL (228.34 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2834 mL

11.4171 mL

22.8342 mL

5 mM

0.4567 mL

2.2834 mL

4.5668 mL

10 mM

0.2283 mL

1.1417 mL

2.2834 mL

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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: 5% DMSO 10% Cremophor EL 85% ddH2O

Solubility: 20 mg/mL (45.67 mM); Suspended solution; Need ultrasonic

Protocol 2

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline

Solubility: 2.5 mg/mL (5.71 mM); Suspended solution; Need ultrasonic

Protocol 3

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (5.71 mM); Suspended solution; Need ultrasonic

Protocol 4

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

Solubility: 2.08 mg/mL (4.75 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.

Protocol 5

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.08 mg/mL (4.75 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 6

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

Solubility: ≥ 2.08 mg/mL (4.75 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Protocolo

Cell Assay^[1]

HEK293 cells are grown in 96-well plates (1×10⁶/well) and are transiently transfected using Lipofectamine. Cells are transfected with a total of 200 ng of DNA per well consisting of the pGL4 mIL-17 firefly luciferase reporter construct, the pGL4 mIL-17 + CNS-5 firefly luciferase reporter construct, or the pGL4 mIL-17 2kB RORE mutant (100 ng/well) , an actin promoter Renilla reniformis luciferase reporter (50 ng/well), and either control vector alone or the test DNA (full-length RORα or full-length RORγ at 50 ng/well). All 48 human nuclear receptors are represented in the specificity assay and SR9009 is tested at a concentration of 20 μM. The format of the assay is a cotransfection assay with Gal4 DNA binding domain-nuclear receptor fusions in HEK293 cells^[1].

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

Animal Administration^[1]

Mice^[1]
For circadian gene expression experiments male C57BL6 mice (8-10 weeks of age) are either maintained on a L:D (12h:12h) cycle or on constant darkness. At circadian time (CT) 0 animals are administered a single dose of 100 mg/kg SR9009 or SR9011 (i.p.) and groups of animals (n=6) are sacrificed at CT0, CT6, CT12 and CT18. Gene expression is determined by real time QPCR.

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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (282 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Solt LA, et al. Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. Nature. 2012 Mar 29;485(7396):62-68. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2834 mL	11.4171 mL	22.8342 mL	57.0854 mL
	5 mM	0.4567 mL	2.2834 mL	4.5668 mL	11.4171 mL
	10 mM	0.2283 mL	1.1417 mL	2.2834 mL	5.7085 mL
	15 mM	0.1522 mL	0.7611 mL	1.5223 mL	3.8057 mL
	20 mM	0.1142 mL	0.5709 mL	1.1417 mL	2.8543 mL
	25 mM	0.0913 mL	0.4567 mL	0.9134 mL	2.2834 mL
	30 mM	0.0761 mL	0.3806 mL	0.7611 mL	1.9028 mL
	40 mM	0.0571 mL	0.2854 mL	0.5709 mL	1.4271 mL
	50 mM	0.0457 mL	0.2283 mL	0.4567 mL	1.1417 mL
	60 mM	0.0381 mL	0.1903 mL	0.3806 mL	0.9514 mL
	80 mM	0.0285 mL	0.1427 mL	0.2854 mL	0.7136 mL
	100 mM	0.0228 mL	0.1142 mL	0.2283 mL	0.5709 mL

Keywords

SR9009

39 Cited Publications

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SR9009

Publications Citing Use of MedChemExpress (MCE) SR9009

Actividad biológica

Chemical Information

Publications (39)

Solvente y solubilidad

Protocolo

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

SR9009 Related Classifications

HY-16989 Related Classifications